Inventi Rapid: Med Chem

Inventi:prmc/31567/21

Synthesis of Novel 2,5-Disubstituted 1,3,4-Thiadiazole for their Potential Anticonvulsant and Antimicrobial Screening: Pharmacophore Model Studies

The 1,3,4,-Thiadiazole nucleus is a ubiquitous feature of many pharmacological activities, as anti-TB, anti-inflammatory,anti-bacterial, anti-oxidizing agents, anti-fungal, anti-cancer, anticonvulsant and antidepressants activity. It could be evidence from literature that substituted hydrazones derivative of 1,3,4-thiadiazole is not reported. Thus in the present study we synthesized novel 2,5-disubstituted 1,3,4-thiadiazole derivatives and it is expected that these derivative would have potent anticonvulsant and antimicrobial activity. The derivatives were characterized by physico-chemical (TLC and Melting Point) and spectral analysis (I.R. Spectroscopy) and finally the biological activities were performed by using different animal models like pentylenetetrazole-induced convulsions in rats for Anti-Convulsant. The compounds P-2(R-Cl, R1-C6H7N3O), P-3(R-OCH3, R1-C6H7N3O), P-5(R-Cl, R1-C7H8N2O), P-6(R-OCH3, R1-C7H8N2O) and P-7(R-NO2, R1-C6H7N3O) showed potent anticonvulsant activity as compare to the standard drug diazepam. And antimicrobial activity were also tested for their anti bacterial activity against gram positive bacteria S. aureus and B. antracis while gram negative bacteria P. aeruginosa and E. coli. And same compounds were tested for their anti fungal activity against C. albicans and A. niger using cup plate method. Streptomycin, erythromycin, fluconazole and ketoconazole were used as a reference compound. The entire compounds shown good activity against gram positive and gram negative bacteria. The compounds P-1(R-H, R1-C6H7N3O), P-2(R-Cl, R1-C6H7N3O), P-4(R-H, R1-C7H8N2O) show moderate activity while P-3(R-OCH3, R1-C6H7N3O), P-5(R-Cl, R1-C7H8N2O), P-6(R-OCH3, R1-C7H8N2O), P-7(R-NO2, R1-C6H7N3O) and P-8(R-NO2, R1-C7H8N2O) show good anti fungal and anti bacterial activities....