SYNTHESIS OF NOVEL ANTIMICROBIAL DERIVATIVES OF 3-SUBSTITUTED PYRROLIDINE2, 5-DIONES USING PHARMACOPHORE HYBRID APPROACH: PART-I

Smita Pawar, Sanjay Sawant, Amit Nerkar, Ashok Bhosale
unpublished
Objective: A series of substituted benzo[d]thiazol-2yl-3-substituted pyrrolidine 2,5-dione compounds, P(1-18) were synthesized and evaluated for their antimicrobial activity against gram positive, gram negative bacteria and fungi. Methods: Titled compounds were synthesized by fusion reaction. The minimum inhibitory concentration was determined using two fold dilution method. The batch grid docking was performed to analyze the probable interactions of synthesized compounds with DNA gyrase.
more » ... s: The compound, P14 was found to be active against E. coli and S. aureus at 3.125 and 6.25µg/ml MIC respectively and compound P15 was found to be active against S. epidermis and E. coli at 6.25 and 3.125 µg/ml MIC respectively. The compound P6, P12, and P18 were found to possess MIC at 6.25 and 12.5µg/ml. Conclusion: Though, the relationship between the activities shown by these compounds in, in vivo and in vitro study is still to be established, these results suggest the suitability of the designed molecular framework as a potential anti-microbial lead.
fatcat:fkmuuhv6sbe4nkf5jbryzcp33u