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 MoreContact:86-574-26865651
Address:529 YuanBaoShan Road, Beilun District
Xiamen Kaijia Imp & Exp Co., Ltd.
Contact:86-592-5101177
Address:Room406 Luhui Building No. 65 Haitian Road Huli Xiamen,China.
ZhangJiaGang YaRui Chemical Co.,Ltd.
Contact:0512-58360968
Address:China JiangSu Province Zhang Jia Gang City YangShe Oriental Plaza Building 10 B307
Evergreen Chemical Industry Ltd.
Contact:86-553-4918210
Address:6#2-602 Wanhaobailing
Tianjin Realet Chemical Technology Co.,Ltd.
website:http://www.realetchem.com
Contact:+86-022-58788819
Address:shuanggang industrial park
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)