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

作者：Chandna Nisha^*; Kapoor Jitander K; Goyal Varsha; Aggarwal Neeraj K; Kumari Kotni Meena; Vijjulatha Manga

来源：Current Topics in Medicinal Chemistry, 2013, 13(16): 2062-2075.

• 1,3-Oxazolidin-2-one
• Azomethine
• Antibacterial activity
• Antifungal activity
• Docking study

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.

• 出版日期2013-8