Bioorganic and Medicinal Chemistry p. 6267 - 6272 (2017)
Update date:2022-08-30
Topics:
Christoff, Rebecca M.
Murray, Gerald L.
Kostoulias, Xenia P.
Peleg, Anton Y.
Abbott, Belinda M.
With multidrug resistant bacteria on the rise, novel antibiotics are becoming highly sought after. In 2008, eleven compounds were identified by high throughput screening as inhibitors of BasE, a key enzyme of the non-ribosomal peptide synthetase pathway found in Acinetobacter baumannii. Herein, we describe the preparation of four structurally similar heterocyclic lead compounds from that study, including one 1,2,5-oxadiazole. A further library of 30 analogues containing the oxadiazole moiety was then generated. All compounds were screened against Acinetobacter baumannii and their minimum inhibitory concentration data is reported, with (E)-3-(2-hydroxyphenyl)-N-(4-methyl-1,2,5-oxadiazol-3-yl)acrylamide 32 found to have an MIC of 0.5 mM. This work provides the foundation for further investigation of 1,2,5-oxadizoles as novel inhibitors of A. baumannii.
View MoreContact:+86-21-61318535
Address:Building 29,No.2139 Xizha Road, Fengxian District, Shanghai
Shanghai Xinda Pharmaceuticals Co., Ltd.
Contact:86-21-33692333-8008
Address:999 Linxian Road, Jinshan Industrial Park, Shanghai, China
ChangZhou XiaQing Chemical Co., Ltd.
Contact:+86-519-88721665
Address:3# Hengluo Road, Henglin Town, Changzhou City, Jiangsu Province,China
SHAANXI TOP PHARM CHEMICAL CO.LTD
Contact:+86-029-85733403
Address:No.108 ,west sector,south er huan,xi'an,china
website:http://www.lonwinchem.com
Contact:Tel: 86-21-59858395
Address:No#966,Huaxu Road,Shanghai 201702,P.R.China
Doi:10.1039/jr9340000218
(1934)Doi:10.1016/S0022-0728(79)80053-4
(1979)Doi:10.1007/BF00457999
(1956)Doi:10.1055/s-0032-1317018
(2012)Doi:10.1016/j.poly.2019.114128
(2019)Doi:10.1016/j.apcata.2016.03.012
(2016)