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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Design, Synthesis and Antimicrobial Evaluation of Novel 1,3-Oxazolidin-2- one Derivatives

Author(s): Nisha Chandna, Jitander K. Kapoor, Varsha Goyal, Neeraj K. Aggarwal, Kotni Meena Kumari and Manga Vijjulatha

Volume 13, Issue 16, 2013

Page: [2062 - 2075] Pages: 14

DOI: 10.2174/15680266113139990132

Price: $65


A series of novel derivatives of 1,3-oxazolidin-2-one 12a-12n has been synthesized starting from 4-nitro-(L)- phenylalanine by involving five-step reaction sequence. All the compounds were screened for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative) and in vitro antifungal activity against two pathogenic fungal strains namely, Candida albicans and Saccharomyces cerevisiae. All the synthesized compounds showed activity against Gram-positive bacteria. Compounds 12c and 12l exhibited maximum antibacterial activity against Gram-positive bacteria. However, against Gram-negative bacteria only five of screened compounds were found to be active. Compounds 12c and 12i displayed best antifungal activity against the tested fungi. Docking studies were carried out in order to gain insight into the mechanism of action and the binding mode of these compounds. These studies were in agreement with the biological data.

Keywords: 1, 3-Oxazolidin-2-one, Azomethine, Antibacterial activity, Antifungal activity, Docking study.

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