title: Synthesis and Antibacterial Evaluation of (S,Z)-4-methyl-2-(4-oxo-5-((5-substituted phenylfuran-2-yl) methylene)-2-thioxothiazolidin-3-yl)Pentanoic Acids.
abstract: The microbial resistance has become a global hazard with the irrational use of antibiotics. Infection of drug-resistant bacteria seriously threatens human health. Currently, there is an urgent need for the development of novel antimicrobial agents with new mechanisms and lower levels of toxicity. In this paper, a series of (S ,Z)-4-methyl-2-(4-oxo-5-((5-substitutedphenylfuran-2-yl) methylene)-2-thioxothiazolidin-3-yl)pentanoic acids via a Knoevenagel condensation were synthesized and evaluated for their antibacterial activity in - vitro. The synthesized compounds were characterized by IR, (1)H NMR and MS. The antibacterial test in - vitro showed that all of the synthesized compounds had good antibacterial activity against several Gram-positive bacteria (including multidrug-resistant clinical isolates) with minimum inhibitory concentration (MIC) values in the range of 2-4 µg/mL. Especially compounds 4c, 4d, 4e and 4f were the most potent, with MIC values of 2 µg/mL against four multidrug-resistant Gram-positive bacterial strains.
authors.affiliation: Medical College, Jinggangshan University, Ji'an, Jiangxi, 343009, China.
authors.forename: Ming-Xia
authors.initials: MX
authors.lastname: Song
authors.affiliation: Medical College, Jinggangshan University, Ji'an, Jiangxi, 343009, China.
authors.forename: Xian-Qing
authors.initials: XQ
authors.lastname: Deng
authors.affiliation: Yanbian University College of Pharmacy, Yanji, Jilin, 133002, China .
authors.forename: Zhi-Yu
authors.initials: ZY
authors.lastname: Wei
authors.affiliation: Yanbian University College of Pharmacy, Yanji, Jilin, 133002, China .
authors.forename: Chang-Ji
authors.initials: CJ
authors.lastname: Zheng
authors.affiliation: Yanbian University College of Pharmacy, Yanji, Jilin, 133002, China .
authors.forename: Yan
authors.initials: Y
authors.lastname: Wu
authors.affiliation: Department of Respiaratory Medicine, Yanbian University Affiliated Hospital , Yanji, Jilin, 133002, China .
authors.forename: Chang-Shan
authors.initials: CS
authors.lastname: An
authors.affiliation: Yanbian University College of Pharmacy, Yanji, Jilin, 133002, China .
authors.forename: Hu-Ri
authors.initials: HR
authors.lastname: Piao
keywords: Antibacterial activity; Cytotoxicity; Furan; MRSA; Pentanoic acid; QRSA