Chinese Journal of Chemistry p. 1111 - 1115 (2020)
Update date:2022-08-17
Topics:
Kong, Xue-Qing
Wei, Bing-Yan
Yu, Chen-Xi
Guan, Xiang-Na
Ma, Wei-Ping
Liu, Gang
Yang, Cai-Guang
Nan, Fa-Jun
To combat multidrug-resistant Gram-positive bacteria, new antimicrobials particularly those with novel mechanism of action are badly needed. Different with conventional antibiotics which are typical inhibitors, small-molecule activators of bacterial ClpP represent a new class of antibiotics. No ClpP activator has been developed for clinical trial. Herein, we conducted a screening on our library of bengamide-like ring-opened analogues and found that L472-2 possesses a low minimum inhibitory concentration (MIC) against S.aureus and shows no activity for ClpP activation in vitro, but it displayed reduced antibacterial activity against S. aureus with clpP deletion. In order to obtain bengamide analogues that activate ClpP in vitro as well as possess antibacterial activity, we perform further structural modifications starting from L472-2. Compound 37 remains the antimicrobial activity and activation of ClpP protein in vitro, which could be viewed as a new chemical scaffold for ClpP activators and worthy of further investigation.
View MoreMedicalChem(Yancheng)Manuf.Co.,Ltd.
Contact:+86-515-84383366
Address:Touzeng BinHai, YanCheng City, JiangSu Province, China
Contact:86-371-63655023
Address:No.85,jinshui road,zhengzhou,China
HANGZHOU YUNUO CHEMICAL CO.,LTD
website:http://www.yunuochem.com
Contact:0571-83715115
Address:hangzhou
Guangzhou Chemical Reagent Factory
Contact:+86-20-8435 9820 or 8435 7345
Address:Southern Guangzhou, Guangdong, China
Hunan Dinuo Pharmaceutical Co.,Ltd.
Contact:86-731-88280100*8561
Address:Bio-pharmaceutical industrial park, Liuyang, Hunan, China
Doi:10.1021/om050325u
(2005)Doi:10.1021/acs.orglett.6b00161
(2016)Doi:10.1016/0009-2614(84)85392-0
(1984)Doi:10.1016/j.apcata.2017.06.015
(2017)Doi:10.1021/acs.orglett.6b01279
(2016)Doi:10.1016/j.bmc.2008.03.054
(2008)