Bioorganic and Medicinal Chemistry p. 6134 - 6145 (2014)
Update date:2022-08-29
Topics:
Pedgaonkar, Ganesh S.
Sridevi, Jonnalagadda Padma
Jeankumar, Variam Ullas
Saxena, Shalini
Devi, Parthiban Brindha
Renuka, Janupally
Yogeeswari, Perumal
Sriram, Dharmarajan
A series of twenty seven substituted 2-(2-oxobenzo[d]oxazol-3(2H)-yl)acetamide derivatives were designed based on our earlier reported Mycobacterium tuberculosis (MTB) enoyl-acyl carrier protein reductase (InhA) lead. Compounds were evaluated for MTB InhA inhibition study, in vitro activity against drug-sensitive and -resistant MTB strains, and cytotoxicity against RAW 264.7 cell line. Among the compounds tested, 2-(6-nitro-2-oxobenzo[d]oxazol-3(2H)-yl)-N-(5-nitrothiazol-2-yl)acetamide (30) was found to be the most promising compound with IC50 of 5.12 ± 0.44 μM against MTB InhA, inhibited drug sensitive MTB with MIC 17.11 μM and was non-cytotoxic at 100 μM. The interaction with protein and enhancement of protein stability in complex with compound 30 was further confirmed biophysically by differential scanning fluorimetry.
View MoreXi'an caijing Opto-Electrical Science & Technology Co., LTD
Contact:+86-29-88294447
Address:NO.168 Zhangba Rd. East, Xi'an, P.R.China
Contact:0091-265-2313036
Address:311, ATLANTIS HEIGHTS SARABHAI MAIN ROAD,VADIWADI ,VADODARA
CHANGZHOU HANGYU PHARMACEUTICAL TECHNOLOGY CO., LTD
website:http://www.czyys.com
Contact:0086-519-88802789
Address:No.300,Yanling Middle Road, Changzhou, Jiangsu, China
Shandong Yaroma Perfumery Co., Ltd.
Contact:+86- 531- 88024598
Address:7-702 Caizhi Central, 59 Gong Ye South Road, Jinan City,250101, P. R. China
Shanghai Mio Chemical Co., Ltd
Contact:0086 21- 64401188-622
Address:16 Floor NO.2 Jiefang Building, No. 4855 Dushi Road, 201100 Shanghai, P.R.China
Doi:10.1002/jps.2600690728
(1980)Doi:10.1007/s10593-019-02448-y
(2019)Doi:10.1016/S0040-4020(01)82311-5
(1991)Doi:10.1021/acs.orglett.9b02393
(2019)Doi:10.1039/c7ta10976h
(2018)Doi:10.1021/ic50175a020
(1977)