Background: In many cases, drugs can exist in more than one crystalline form; the phenomenon is known as "polymorphism." Though the polymorphs are chemically identical, they exhibit different physicochemical properties, viz., melting point, solubility, X-ray diffraction pattern, etc., which further affect the biological properties of drugs. The purpose of this work was to study the effect of solvents on crystallization, solubility and dissolution of rofecoxib and celecoxib. Materials and Methods: The crystals were prepared by using different solvents. The melting point, solubility, dissolution, Fourier-transformed infrared (FT-IR), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM) studies were carried out to confirm the polymorphism in drugs. Result: The results indicate that the crystals obtained from different solvents exhibited different physicochemical properties. Though FT-IR and XRD gave an indication of different crystal morphs, DSC proved absence of any polymorphic behavior in the crystals of rofecoxib and celecoxib. Conclusion: Crystals having the desired physicochemical properties may be obtained by selecting solvents of specific polarities.

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Background and Aim: Closely related plant species often share similar secondary metabolites and bioactivities and are therefore good targets for bioactivity testing when one or more species within a genus are known to possess therapeutic properties. The genus Aloe has a long history of medicinal usage in many areas of the world. Many species are known to have therapeutic properties, several species of which have well-established antibacterial bioactivities. The current studies examine the toxicity of several Aloe species and their ability to inhibit bacterial growth and compare them to the most extensively studied species, Aloe barbadensis, which has well-established antibacterial bioactivities. Results: A. barbadensis methanolic extract displayed broad spectrum antibacterial activity, inhibiting the growth of 8 of the 14 bacteria tested (57%). It was effective against both Gram-positive and Gram-negative bacteria, inhibiting the growth of 4 of 4 Gram-positive bacteria (100%) and 4 of 10 Gram-negative (40%) bacteria tested, respectively. In contrast, Aloe elgonica, Aloe pruinosa, Aloe chabaudii, Aloe daiyana, Aloe marlothi and Aloe vryheidensis all showed no antibacterial activity toward any of the bacteria tested. All of the Aloe species displayed low toxicity similar to that of the A. barbadensis control. A. daiyana was the most toxic of the Aloe species tested with 24, 48 and 72 hours LC50 values of 1018.2, 517.0 and 405.7 ΅g/ml, respectively. Conclusions: Despite their close taxonomic relationship, A. elgonica, A. pruinosa, A. chabaudii, A. daiyana, A. marlothi and A. vryheidensis do not have the same antibacterial medicinal potential as A. barbadensis, but may still have other similar toxicity-related bioactivities. Testing against protozoa, fungi, virus and tumor cells is required to determine if this is the case.

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The leaf of Costus pictus D. Don is considered as an antidiabetic in folklore medicine and is known to reduce the blood sugar, similar to insulin. The aim of this study is to investigate the effect of ethanolic extract of C. pictus leaf on glucose uptake by L6 myotube cell line (skeletal muscle cells) involved in glucose utilization. Ethanolic extract of C. pictus leaf was analyzed to study GLUT4 translocation and glucose uptake activity, but it has no direct peripheral action at 300 μg/ml dose comparable with insulin and metformin. The glucose uptake was not enhanced by the extract of C. pictus leaf.

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Introduction: The dry powdered leaf of Vernonia galamensis (Asteraceae) has been used by traditional herbalists in northern Nigeria to treat diabetes mellitus. However, medicinal plants used in folk medicine have no standard dose or acceptable method of formulation. In this study therefore, the leaves of Vernonia galamensis (Asteraceae) were extracted, evaluated for pharmacological activity and formulated into tablets. Materials and Methods: The extract was found to be highly hygroscopic and deliquescent, therefore the following efflorescent diluents; aerosil® 200 (GmbH, Meggle, Germany), avicel PH 101 (Honey Well and Stein, UK), and anhydrous calcium phosphate (BDH chemicals, England) were used. The wet granulation method was employed for the tablet formulation and the compaction characteristics of the granules were determined using the Heckel equation. Results and Conclusions: Negative intercepts were a setback to the use of the Heckel equation due to the resulting negative values of D _A and D _B . This makes it difficult to explain the compaction characteristics of the crude extract.

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Aims and Objectives : It is observed that negative studies published in medical journals are underpowered to detect the actual difference between the groups, but no data are available on the quality of the statistics reported in these studies. Therefore, this study was carried out with aim of evaluating negative studies published in Indian medical journals for adequacy of reporting of descriptive and inferential statistics. Materials and Methods : All the original articles published in 14 Pubmed-indexed Indian medical journals were analyzed to determine whether the study was negative or positive. All the negative studies were analyzed for correctness of the descriptive statistics and inferential statistics. The types of data and statistical methods were also noted down. Descriptive statistics was used and values were expressed as frequency, percentages and confidence interval. Results : Incorrect descriptive statistics was mentioned in 15 (28.8%, 95% CI 18.3-42.2%) studies. Information related to assumptions of statistical tests were mentioned in only two (3.8%, 95% CI 1.0-12.9%) articles. Inappropriate/incorrect statistical tests was used in 22 (42.3%, 95% CI 29.8-55.8%) studies. The most common reason for inappropriate reporting of descriptive statistics was use of mean and SD for description of ordinal data. The most common reason for incorrect statistical test was use of parametric test for ordinal data. The most common statistical test was the t-test. Conclusion : Negative studies published in prominent Indian medical journals are statistically weak, and readers critically analyze these studies before making any opinion based on them.

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Background: Although initially introduced for the management of hypertension, al-adrenergic-receptor antagonists (a ₁ blockers) have become the standard of care for the medical management of benign prostatic hyperplasia (BPH)-related lower urinary tract symptoms (LUTS). Alpha-blockers (alfuzosin, tamsulosin, doxazosin, prazosin, and terazosin) relax the smooth muscles in the prostate and are indicated for the symptomatic treatment of BPH, due to evidence of their positive and rapid effect on LUTS. Objective: Our objective was to develop and validate a method for simultaneous estimation of these drugs. Our aim was to develop a UV spectrophotometric method because of the simplicity and economical advantage of this technique. Materials and Methods: All these drugs were dissolved in the same solvent (methanol) and scanned under a ShimadzuUV spectrophotomer, under full UV (ultraviolet) range (200 - 400 nm). Result: After some experiments we found that this is impossible. This was evident from our study that UV spectra were overlapping each other, except in the case of tamsulosin. Conclusion: Same class of drugs may have almost the same functional groups, and gradient Reverse-Phase Liquid Chromatography(RPLC) will be more useful to separate such complicated mixtures. Therefore, we propose to develop a gradient High-Performance Liquid Chromatography(HPLC) method as it may be a more suitable method for the simultaneous estimation of these drugs.

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Introduction: Ficus religiosa L. (Moraceae) has been of great medicinal value in traditional medicine and implicated in a wide variety of human and animal disorders. Its leaves have been used for the ethnomedical treatment of epilepsy. But its traditional antiepileptic use is not fully understood experimentally. Hence the present study was undertaken to explore the anticonvulsant effect of the leaves in experimental animal models of convulsion. Materials and Methods: The anticonvulsant effect of hydroethanolic leaf extract of F. religiosa was studied at 100, 250 and 500 mg/kg; intraperitoneally (i.p.) in maximal electroshock (MES), and at 100, 250, 500 and 600 mg/kg; i.p. doses in pentylenetetrazol (PTZ) test in mice. The duration of tonic hind limb extension(s) and latency to clonic convulsions (min) was noted in MES and PTZ tests, respectively. Phenytoin (25 mg/kg; i.p.) and diazepam (5 mg/kg; i.p.) served as reference standards in MES and PTZ tests, respectively. Percentage mortality was also noted. Results: There was no significant change observed after the extract treatment on the duration of tonic hind limb extension in MES test, and latency to clonic convulsions in PTZ test, as compared to their respective controls. Moreover, percentage mortality remained unaltered after the extract treatment. Conclusions: From the results of present study it is concluded that the hydroethanolic leaf extract of F. religiosa lacks anticonvulsant activity in MES- and PTZ-induced convulsion tests. Further studies are required from other regions and using different animal models to support these findings.

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Background: Pyrimidine and fused pyrimidine derivatives play an important role in therapeutic strategies. It is known to be most prominent structures found in nucleic acid, including uracil, thymine, cytosine, adenine, and guanine, which are fundamental building blocks for deoxyribonucleic acid (DNA) and ribonucleic acid (RNA). Materials and Methods: A series of 3-[2-amino-6-(substituted)-pyrimidin-4-yl]-6-(substituted)-2H-chromen-2-one derivatives were prepared by reacting salicylaldehyde with ethylacetoacetate in the presence of piperidine by Knoevenagel reaction as a starting material. The chemical structures were confirmed by means of FTIR (Fourier Transform InfraRed Spectrophotometer-8400S), 1H NMR, and elemental analysis. The data of these synthesized compounds were submitted to National Institute of Health, USA, under the drug discovery program of NCI (National Cancer Institute) and screened for anticancer activity at a single high dose (10−5 M) in full NCI 60 cell lines. Results: Unfortunately, the selected compounds have not shown any potent significant anticancer activity in the NCI 60 cell line screening. Conclusion: The compound (T2) found to be most efficient anticancer activity with selective influence on breast cancer cell lines, especially on MCF7 cell line with a growth percentage of 33.63.

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Objective: The present study evaluates the antibacterial activity (Minimum Inhibitory Concentration- MIC, Minimum Bactericidal Concentration- MBC) and the Fractional Inhibitory Concentration (FIC) of crude extracts and compounds isolated from Miconia rubiginosa against ten clinical bacterial isolates and one standard bacterial strain Expanded-Spectrum β-lactamase (ESBL)-producing enterobacteria. Materials and Methods: The crude extracts were obtained by maceration and the compounds isolated were purified through different chromatography techniques, and then structures were identified for physical methods of organic analysis. The evaluation of the antibacterial activity for the microdiluition in broth technique. Results: The MIC and MBC result for the ethanolic extract was 2.0 mg/mL. For the dichloromethane extract and ursolic acid and oleanolic acid, MIC was >2.0 mg/mL, but no bactericidal activity (MBC) was observed. The FIC values achieved with the combinatioin of the crude extracts with clavulanic acid were not significantly different. Conclusion: The ethanolic extract from Miconia rubiginosa exhibits better antibacterial activity, but the two isolated compounds are not active against the tested bacterial isolates. The combination of the crude extracts with clavulanic acid does not lead to synergism, and there are no statistical differences between the two crude extracts in this sense.

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Objectives: To verify the contribution of N-acetylcysteine (NAC) as an antioxidant drug in the therapy of diabetes, helping to reduce the deleterious effects resulting from oxidative stress associated with the hyperglycemic state. Materials and Methods: The animals were divided into normal (saline, 25 mg/kg NAC, and 75 mg/kg NAC) and diabetic rats (saline, 25 mg/kg NAC, and 75 mg/kg NAC) with five rats per group, and were treated or four weeks. Diabetes induction was performed by intraperitoneal injection of alloxan after fasting for 12 hours. Subsequently, glucose solution was used to promote wear of the pancreatic beta cells. Blood parameters such as glucose, glycated hemoglobin, hepatic and renal biomarkers, and butyrylcholinesterase activity were determined by commercial kits. Catalase, glutathione peroxidase, and superoxide dismutase activities were measured using spectrophotometric techniques, while glutathione and malondialdehyde levels were determined by chromatographic techniques. Results: NAC had no significant differences on glycemic, hepatic, renal, and oxidative stress biomarkers. Superoxide dismutase activity was significantly higher ( P < 0.05) in diabetic rats treated with NAC compared to the diabetic saline group, while butyrylcholinesterase activity was significantly lower ( P < 0.05) in the same groups. There was a negative correlation between superoxide dismutase and butyrylcholinesterase activities. Conclusion: NAC supplementation did not re-establish the antioxidant system and consequently the deleterious effects of diabetes did not decrease. Diabetic groups that received NAC demonstrated that superoxide dismutase activity was indirectly linked to the levels of butyrylcholinesterase. More studies are necessary to investigate the action of NAC on superoxide dismutase and butyrylcholinesterase activities in the diabetic state.

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Objective: Biophytum sensitivum is an important medicinal plant extensively used in traditional oriental herbal medicines. Though medicinal use of this plant is known, the active principles responsible such property is not known. Pharmacological screening of this plant may lead to discovery of new activity with new mode of treatment. Hence, screening for in-vitro pharmacological activities of methanolic callus extracts of Biophytum sensitivum has been carried out. Experiments were designed according to the standard methods and processes. Materials and Methods: Leaf cutting derived callus on MS medium supplemented with BA (Benzyl adenine) 1.0 mg/l + NAA (1-naphthaleneacetic acid) 1.0 mg/l is used as a source, and compounds were extracted from dried callus using methanol solvent with Soxhlet apparatus. Results: The callus extract has shown antioxidant activity, in-vitro inhibition of enzyme activities like α-glycosidase, acetyl cholesterase, and tyrosinase, but potency was found to be low. The Graph pad Prism Version-5 software is used to analyze data in the form of Figures. Conclusion: For the first time, we are reporting in-vitro pharmacological screening of methanolic callus extracts of Biophytum sensitivum.

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Purpose: The aim of the present research is to monitor any alteration in the serum concentrations of lamotrigine (LMT) in peripheral neuropathic conditions compared with normal conditions in a rat model. Materials and Methods: LMT concentrations were established at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h post dose by high performance liquid chromatography-ultraviolet. After per oral administration of 10 mg/kg drug, pharmacokinetic parameters were determined from plasma drug concentration. Later pharmacokinetic parameters of neuropathic pain induced rats were calculated in order to estimate the possible effect of neuropathic pain on pharmacokinetic parameters. Results: The regression coefficient determined for LMT calibration curve was 0.99 ± 0.001. The working range for LMT was 0.5 to 2.5 μg/ml Limit of Detection (LOD 0.2 μg/ml). The maximum drug concentration was found at 2 h. Conclusion: However, none of the pharmacokinetic parameter showed statistically significant alteration where the results were quite stimulating for the development of clinically useful oxcarbazepine dosage form to explore its activity on neuropathic pain.

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Introduction: The use of pharmacological agents in the treatment of anxiety disorders have fallen out of favor as their unwanted side-effects have become evident. These presenting challenges call for an inward look into harnessing the full potential of medicinal plants that abound around us. Aim: This study aimed at evaluating the anxiolytic activity of ethanolic fruit extract of Sarcocephalus latifolius in mice. Materials and Methods: The prepared extract at 200, 400, and 600 mg/kg as well as 2.5 mg/kg of diazepam reference standard was administered orally. Anxiolytic activity of the extract was explored using elevated plus-maze and open-field models. Result: In the elevated plus-maze, the extract possessed insignificant (P > 0.05) anxiolytic effect by decreasing the time spent in open arms and entries into the open arms. However, the time spent in the closed arms increased significantly in the extract treated groups compared to the reference standard. In the open-field model, no significant (P > 0.05) locomotor activity was observed in the extract groups. The number of locomotion was less in the extract groups compared the reference standard having the highest locomotive activity. Furthermore, there were reduction in the number of rearing at extract doses of 400 and 600 mg/kg compared with the normal saline and reference standard. Conclusion: The results of this study showed that the ethanolic fruit extract of S. latifolius lack anxiolytic activity.

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Background: Organismal performance assays (OPAs) are a unique method of toxicity quantification used to assess the safety of potentially toxic compounds such as pharmaceuticals. OPAs utilize genetically diverse wild mice (Mus musculus) housed in large seminatural enclosures wherein exposed individuals compete directly with controls for resources. Previously, OPAs have been successful in detecting adverse effects in mice that were exposed to paroxetine. Here, we further test OPAs' utility in pharmaceutical safety assessment by testing OPAs with rofecoxib, a drug with known adverse effects on humans. Materials and Methods: We exposed mice to rofecoxib (~37.5 mg/kg/day) during gestation and into early adulthood. Exposure ceased when individuals were released into enclosures. Five independent populations were established and rofecoxib-exposed individuals (n = 58) competed directly with control individuals (n = 58) over 28 weeks. Organismal performance was determined by quantifying reproduction, survival, and male competitive ability. Results: In enclosures, rofecoxib-exposed males had equal reproduction, survival, and competitive ability. Rofecoxib-exposed females had equal survival compared to controls but experienced 40% higher reproductive output. Conclusions: The adverse health effects of rofecoxib seen in humans escaped detection by OPAs, just as they had during traditional preclinical assays. These results may be explained by the exposure design (in the enclosures, all animals were on the control diet), the relatively short duration of exposure, species differences, or because the health benefits of the drug negated the side effects. Similar to numerous assays used in preclinical trials, OPAs cannot reveal all maladies, despite their demonstrated sensitivity in detecting cryptic toxicity from numerous exposures.

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Aims: Withania somnifera is widely employed as a rejuvenator and expected to promote physical health and increase longevity. The aim of the present research work was to evaluate Cytochrome P450 3A (CYP3A) interaction of Withania somnifera. Materials and Methods: In vitro CYP3A interaction of methanolic extract of Withania somnifera (WS) and its principal phytoconstituents: Withaferin-A (WA), Withanolide-A (WL-A) and Withanoside-IV (WS-IV) were investigated in rat and human liver microsomes. In vivo CYP3A interaction potential was investigated by administering methanolic extract of WS orally at a dose of 500 mg/kg in female Wistar rats. Sildenafil citrate was used to index the activity of CYP3A. Results: IC ₅₀ values of methanolic extract of Withania somnifera, WA, WL-A, WS-IV were found to be 200 μg/ml, >20 μM, >64 μM and >64 μM for CYP3A both in rats and humans, respectively. When sildenafil citrate was orally co-administered with methanolic extract of WS and compared with orally administered sildenafil citrate alone, the area under plasma concentration time (AUC) curve and C _max did not significantly differ as compared to the group which received rifampicin orally (positive control). Conclusions: Results suggested that methanolic extract of WS, WA, WL-A, WS-IV showed no in vitro CYP3A inhibition in rats and humans. Methanolic extract of WS did not significantly alter the pharmacokinetics of sildenafil citrate in rats; indicating its safety when co-administered with other drugs that are substrates of CYP3A. Thus the results indicate the lesser likelihood of drug herb interactions when concomitantly administered with CYP3A substrates.

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Objective: The objective of the present study was to investigate the antimicrobial activity of seed of Santalum album Linn. (Family: Santalaceae) in various microbial strains. Materials and Methods: The effects of ethanolic extract of seed of S. album were analyzed in different microorganisms at a concentration of 5 mg/ml per disk. Results: The result indicated that the ethanolic extract of seed of S. album did not show any zone of inhibition against the tested microorganisms. Conclusion: The ethanolic extract of seed of S. album has no significant antimicrobial activity.

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Objective: To investigate the antiglycation potential of fresh juice of whole plant of Enicostema axillare (Lam.) Raynal. in vitro. Materials and Methods: Antiglycation activity of fresh juice of whole plant was determined in vitro using five concentrations (25, 50, 100, 200, and 400 μg/ml) by determining their ability to inhibit the formation of advanced glycation endproducts in a bovine serum albumin / glucose system using fluorescence spectroscopy. Results: There is no antiglycation activity in vitro of fresh juice of E. axillare plant. Conclusion: It is unlikely that impairment of diabetic complications by E. axillare whole plant juice as claimed by ayurvedic and traditional physicians is mediated via antiglycation activity.

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Background and Aim: It is observed that negative clinical trials published in medical journals are poor in reporting of sample size calculation, various components of calculation of sample size. It is also observed that they are underpowered to detect the actual difference between the treatment outcomes. Because of scarcity of these data for Indian medical journals we designed this study to critically analyze the Indian medical journals for reporting of sample size, components of sample size and power. We calculated post hoc power for 30% and 50% difference between the treatment outcomes. Materials and Methods: All the negative clinical trials published in five Indian medical journals (Indian Journal of Pharmacology (IJP), Indian Pediatrics (IP), Indian Journal of Dermatology (IJD), Indian Journal of Dermatology, Vanereology and Leprology (IJDVL), and Journal of Postgraduate Medicine (JPGM)), between 2001 and 2008, were analyzed by each author for reporting of the sample size and components of the sample size. Post hoc power for 30% and 50% differences between the outcome was calculated by G Power software. All data were expressed as frequency, percentages, and 95% confidence interval around the percentages with the help of SPSS ver. 17. Results: The median sample size was observed to be 33 (range 9-85). Power was calculated in 28 (41.1%, 95% CI 30.2% to 53%) trials. The sample size was not calculated in 34 (50%, 95% CI 38.4% to 61.5%) trials. The full sample size was calculated in only 2 (2.9%, 95% CI 0.8% to 10.1%) trials. Post hoc power above 80% for 30% of difference was reported in 3 (4.4%, 95% CI 1.5% to 12%) trials and for 50% difference in outcome it was reported in 42 (61.7%, 95% CI 49.8% to 72.3) trials. Conclusion: Negative clinical trials published in five Indian journals are poor in reporting of sample size calculation. It is also observed that most of trials are underpowered to see the 30% and 50% difference between the outcomes. There is a need to generate more awareness regarding the sample size and power calculation

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Background and Aim: Azadirachta indica has a long history of medicinal usage in skin ailments due to its antibacterial and anti-inflammatory properties. The present study was undertaken to explore the potential of the leaves and bark of Azadirachta indica in the treatment of acne. Materials and Methods: Monographic analysis of the plant was carried out, followed by the phytochemical screening of the sequential extracts of leaves and bark of Azadirachta indica. The results indicated presence of alkaloids, flavonoids, saponins, terpenes, and tannins. Gas chromatography-mass spectrometry (GC/MS) analysis of the test extracts indicated the presence of many phytoconstituents in dichloromethane and methanolic extracts namely stigmasterol, nimbiol, sugiol, 4-cymene, α-terpinene terpinen-4-ol, and vitamin E. The test extracts were evaluated against acne causing bacteria, namely Staphylococcus aureus (MTCC 96), Staphylococcus epidermidis (MTCC 2639), and Propionibacterium acnes (MTCC *1951), for their in vitro antimicrobial activity, using agar disc diffusion method. Results: Dichloromethane and methanolic extracts of Azadirachta indica showed very little activity against S. aureus and S. epidermidis, but did not show any antimicrobial activity against P. acnes. Conclusion: Despite possessing antibacterial properties, Azadirachta indica showed insignificant effect against acne causing bacteria.

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Introduction: Glycation, one of the post-translational modifications of proteins, is a nonenzymatic reaction initiated by the primary addition of sugar to the amino groups of proteins. In the early stage of glycation, the synthesis of intermediates leads to the formation of Amadori compounds. In the late stage, advanced glycation end products (AGE) are irreversibly formed after a complex cascade of reactions. It has recently become clear that glycation also affects diabetes-related complications and Alzheimer's disease. The main aim of this investigation is to provide direct evidence for the effects of Noscapine on HSA glycation. Materials and Methods: In this study human serum albumin (HSA) (10 mg / ml) was incubated in phosphate buffered saline (PBS) (50 mM) with Glucose (40 mM) and different concentrations of Noscapine (25, 100, 250, 500 μM), for 42 days, at 37°C, as also HSA was incubated alone (control or H), with Glucose (40mM) (glycated or H + G), respectively, under the same conditions. After incubation the samples were prepared for circular dichroism (CD) and Fluorescencetechniques. Statistical Analysis Used: The results were expressed as mean ± SEM and chi square test was significant at P < 0.05. Results: In glycated sample CD and Fluorescence showed more change relative to the control sample, but in the presence of different Noscapine concentrations and Glucose there were no significant changes relative to the glycated sample. Conclusions: Thus, this study suggests that Noscapine is not responsible for the antiglycation effect.

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Introduction: Sphaeranthus indicus Linn, an asteracid weed, has been studied by various researchers. The flower of S. indicus possesses biological activities like Nematicidal, Larvicidal, Piscicidal and others, for example, agricultural. Objective: The present investigation for the antiprotozoal activitiy of a methanolic extract (MeOHx) and the alkaloidal fraction (SAF) of the flowers of Sphaeranthus indicus Linn. has been undertaken. Materials and Methods: The study was carried out in seven groups of the Paramecium sp. by using the hemocytometer technique. Different concentrations of MeOHx (50 and 100 μg / ml) and SAF (20 and 40 μg / ml) were applied. The percent mortality was calculated and the results were expressed by using the probit analysis. Results: There was no significant activity against the tested protozoa. Conclusion: Thus, the results of the present investigation suggest that MeOHx and SAF are not responsible for the antiprotozoal property of S. indicus.

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By reacting maleic anhydride with amines, we synthesized the derivatives N-ethyl, N-(2-ethylamine), N-piperidinyl, N-phenyl, and N-phenylhydrazinyl maleamic acids. The purity of these products was initially verified by melting range and the presence of only one spot observed by thin layer chromatography. The chemical structures of the obtained N-alkyl maleamic acids were confirmed through infrared (IR) and hydrogen and carbon nuclear magnetic resonance ( ¹ H and ¹³ C NMR) spectrometry. Due to the already proven pharmacological activity of maleimides, maleic anhydride and its N-alkyl maleamic acids were subjected to in vitro assays to observe antiviral (SA-11 rotavirus), antibacterial (Escherichia coli, Staphylococcus aureus, and Bacillus cereus), antifungal (Colletotrichum musae, Fusarium solani f. sp. phaseoli, Fusarium solani f. sp. piperis Alb., and Penicillium sp.), and antiprotozoal (Trichomonas vaginalis, Giardia lamblia, and Entamoeba histolytica) effects. To study the anti-rotavirus properties, firstly the 3-(4,5-dimethylthiazol-2-yl)-2-5-diphenyltetrazolium bromide (MTT) method was used to establish the median cytotoxicity concentration (CC ₅₀ ) of the compounds, using MA-104 cell line. Under the experimental conditions used, cytotoxic, anti-rotavirus, antibacterial, and antifungal properties were not observed for these compounds.

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Aim: It was aimed to synthesise some novel thiazolidinone derivatives and assess them for antidiabetic activity. Material and Methods: A series of substituted 5-ethylidene-2-(phenylimino) thiazolidin-4-ones were prepared by using phenylthiourea (I) as a starting material. Phenylthiourea on reaction with ethylchloroacetate, in the presence of ethanol and fused sodium acetate, gave 2-(phenylimino) thiazolidin-4-one (II), and 2-(phenylimino) thiazolidin-4-one on further reaction with substituted benzaldehyde gave substituted 5-ethylidene-2- (phenylimino) thiazolidin-4-one (III - XVIII). The synthesized compounds were authenticated on the basis of elemental analysis, IR, 1H NMR, and Mass spectral analysis and some of the compounds were selected on the basis of a literature review, to evaluate them for their antidiabetic activity. Results and Conclusion: All The tested compounds 5-(4-fluorobenzylidene)-2-(phenylimino) thiazolidin-4-on (VII) and 5-(4-Methylbenzylidene)-2-(phenylimino)thiazolidin-4-one (X), 5-(2, 4-dinitrobenzylidene)-2-(phenylamino) thiazolidin-4-one (XVII) were found to be ineffective in lowering the blood glucose level.

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