Synthesis And Evaluation Of Antitubercular Activity Of Novel N-Cyclohexyl-5-Phenyl-1, 3, 4-Thiadiazol-2-Amine Derivatives

Abstract

Background: In current era the wing of innovative therapeutic molecules i.e hybrid molecules synthesis, which comprises of linking two or more therapeutically verified molecules has gained wide appreciation. It was established that, when one heterocyclic system is attached to one more heterocyclic system, superior biological activity was produced. On basis of this important biological activity profile of several thiadiazoles, we intended to synthesize and evaluate the antimycobacterial activity of novel fused cyclohexylamine 1, 3, 4-thiadiazoles derivaties (C_1-5).

Materials and Methods: A series of compounds titled N-Cyclohexyl-5-phenyl-1, 3, 4-thiadiazole-2-amine derivatives (C₁-C₅) are synthesized using appropriate synthetic procedure and characterized by using IR.1NMR, Mass & Elemental analysis. All the thiadiazole amines (C_1-5) were tested for their antimycobacterial activity against M.tuberculosis H37 RV strain.

Results: The tested compounds showed significant antimycobacterial activity. At 1.6µg/ml, compound C₅ shoewd excellent activity against M.tuberculosis H37 RV strains and compound C₁ exhibited good antitubercular activity at 3.12µg/ml.

Conclusion: Compounds bearing the electron donating groups at 4^th position were found to possess excellent antitubercular activity, the substitution on phenyl ring was found to enhance the potentiality of the pharmacophoric moiety.