Abstract
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.
Current Topics in Medicinal Chemistry
Title:Design, Synthesis and Antimicrobial Evaluation of Novel 1,3-Oxazolidin-2- one Derivatives
Volume: 13 Issue: 16
Author(s): Nisha Chandna, Jitander K. Kapoor, Varsha Goyal, Neeraj K. Aggarwal, Kotni Meena Kumari and Manga Vijjulatha
Affiliation:
Keywords: 1, 3-Oxazolidin-2-one, Azomethine, Antibacterial activity, Antifungal activity, Docking study.
Abstract: 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.
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Cite this article as:
Chandna Nisha, Kapoor K. Jitander, Goyal Varsha, Aggarwal K. Neeraj, Kumari Meena Kotni and Vijjulatha Manga, Design, Synthesis and Antimicrobial Evaluation of Novel 1,3-Oxazolidin-2- one Derivatives, Current Topics in Medicinal Chemistry 2013; 13 (16) . https://dx.doi.org/10.2174/15680266113139990132
DOI https://dx.doi.org/10.2174/15680266113139990132 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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