title: Synthesis and antibacterial evaluation of rhodanine-based 5-aryloxy pyrazoles against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA and QRSA).
abstract: With an intention to synergize the anti-bacterial activity of 5-aryloxy pyrazole and rhodanine derivatives, eight series of hybrid compounds have been synthesized and evaluated for their antibacterial activity. The majority of the synthesized compounds showed good inhibitory activity against selected methicillin resistant and quinolone-resistant Staphylococcus aureus (MRSA, QRSA) with minimum inhibitory concentration (MIC) values in the range of 1-32 μg/mL. The cytotoxicity test suggests that these compounds exhibited in vitro antibacterial activity at non-cytotoxic concentrations. These studies therefore suggest that rhodanine-based 5-aryloxy pyrazoles are interesting scaffolds for the development of novel Gram-positive antibacterial agents.
authors: Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, 977 Gongyuan Road, Jilin, Yanji 133002, PR China.
authors: Ming-Xia
authors: MX
authors: Song
authors: Chang-Ji
authors: CJ
authors: Zheng
authors: Xian-Qing
authors: XQ
authors: Deng
authors: Liang-Peng
authors: LP
authors: Sun
authors: Yan
authors: Y
authors: Wu
authors: Lan
authors: L
authors: Hong
authors: Ying-Jing
authors: YJ
authors: Li
authors: Yi
authors: Y
authors: Liu
authors: Zhi-Yu
authors: ZY
authors: Wei
authors: Ming-Jun
authors: MJ
authors: Jin
authors: Hu-Ri
authors: HR
authors: Piao
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015363:Quinolones / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D011720:Pyrazoles; D015363:Quinolones