Bioorganic and Medicinal Chemistry Letters p. 3526 - 3528 (2018)
Update date:2022-07-29
Topics:
Majed, Hiwa
Johnston, Tatiana
Kelso, Celine
Monachino, Enrico
Jergic, Slobodan
Dixon, Nicholas E.
Mylonakis, Eleftherios
Kelso, Michael J.
Methicillin-resistant Staphylococcus aureus (MRSA) is a major cause of serious hospital-acquired infections and is responsible for significant morbidity and mortality in residential care facilities. New agents against MRSA are needed to combat rising resistance to current antibiotics. We recently reported 5-hydroxy-3-methyl-1-phenyl-1H-pyrazole-4-carbodithioate (HMPC) as a new bacteriostatic agent against MRSA that appears to act via a novel mechanism. Here, twenty nine analogs of HMPC were synthesized, their anti-MRSA structure-activity relationships evaluated and selectivity versus human HKC-8 cells determined. Minimum inhibitory concentrations (MIC) ranged from 0.5 to 64 μg/mL and up to 16-fold selectivity was achieved. The 4-carbodithioate function was found to be essential for activity but non-specific reactivity was ruled out as a contributor to antibacterial action. The study supports further work aimed at elucidating the molecular targets of this interesting new class of anti-MRSA agents.
View MoreTianjin Dongchang Fine Chemical Industry Co., Ltd.
Contact:+86-22-29894595
Address:Economic Developing Zone, Ji County, Tianjin, China
Contact:+65 9658 0999
Address:26 Sin Ming Lane, Midview City, #05-118, Singapore 573971
website:http://www.afinechem.com
Contact:+86-571-85134551
Address:No. 206 Zhen Hua Road, Hangzhou 310030, Zhejiang, China
ZHIJIANG ZENVA SINO COMMERCE AND TRADE CO., LTD.
website:http://www.zenvasino.com
Contact:+86-138-72658998
Address:Shibeishan Road,Zhijiang, Hubei, China
Laizhou City Laiyu Chemical CO.,Ltd
Contact:+86-535-2719337/2719339
Address:Chenggang road zhuyou laizhou City Shangdong China
Doi:10.1002/ejoc.201300947
(2013)Doi:10.1021/ol049422u
(2004)Doi:10.1021/ja01152a060
(1951)Doi:10.1021/jo01336a024
(1979)Doi:10.1016/S0040-4020(02)00025-X
(2002)Doi:10.1016/j.tetlet.2012.06.002
(2012)