Synthesis and in silico studies of pyrrolidine sulfonamide based dipeptides as ß-gluscosidase inhibitors.

A series of novel pyrrolidine sulfonamide derivatives were designed, synthesized and screened in silico for their ß-gluscosidase inhibitory activity. The results showed that the pyrrolidine derivatives exhibited moderate inhibitory activity against human ß-gluscosidases inhibitors. The structure-activity relationships were also briefly discussed. The studies indicated that compounds of Series B with imidazole sulfonyl group were the most potent inhibitors compared to the other compounds under investigation.

In vitro microbiological evaluation of novel bis pyrazolones.

Two series of bis pyrazolones (one with 3-methyl substituent and the other one with 3-amino substituent on the pyrazolone ring) were synthesized by the cyclization reaction between various hydrazides with esters/cyano esters in ethanolic medium. Structures of newly synthesized compounds were confirmed by elemental analysis, IR, (1)H NMR and mass spectral data. These compounds were screened for antibacterial and antifungal activities. The compounds of series 3 with amino substituent demonstrated better activity than the compounds of series 2 with methyl substituent on the pyrazolone ring. Compounds "e, f, c and d" showed higher antimicrobial activity than the compounds "b and a". The antimicrobial potentials of the synthesized compounds were compared with that of standards.

Synthesis, characterization and biological studies of substituted quinozoline-4-(3H)-ones containing diazepine moiety.

The synthesis and characterization of new series of 1,4-benzodiazepine derivatives have been presented. The structures were confirmed by elemental analyses, IR spectral, (1)H NMR spectral and mass spectral data. All the compounds were screened for in vitro antimicrobial and anthelmintic activities. The antibacterial activity was tested against Staphylococcus aureus (Gram positive), Bacillus cereus (Gram positive), Escherichia coli (Gram negative) and Pseudomonas aeruginosa (Gram negative). The antifungal activity was tested against Aspergillus niger and Candida albicans. All the compounds showed considerable antimicrobial activity against the microorganism studied. The significant anthelmintic activity of all novel compounds was demonstrated against Pheretima posthuma. Based on the nature of substituent present, the structure-activity correlation of novel compounds was discussed.