European Journal of Medicinal Chemistry p. 539 - 550 (2018)
Update date:2022-08-04
Topics:
Poce, Giovanna
Cocozza, Martina
Alfonso, Salvatore
Consalvi, Sara
Venditti, Giulia
Fernandez-Menendez, Raquel
Bates, Robert H.
Barros Aguirre, David
Ballell, Lluis
De Logu, Alessandro
Vistoli, Giulio
Biava, Mariangela
BM635 is the hit compound of a promising anti-TB compound class. Herein we report systematic variations around the central pyrrole core of BM635 and we describe the design, synthesis, biological evaluation, pharmacokinetic analysis, as well as in vivo TB mouse efficacy studies of novel BM635 analogues that show improved physicochemical properties. This hit-to-lead campaign led to the identification of a new analogue, 4-((1-isopropyl-5-(4-isopropylphenyl)-2-methyl-1H-pyrrol-3-yl)methyl)morpholine (17), that shows excellent activity (MIC = 0.15 μM; SI = 133) against drug-sensitive Mycobacterium tuberculosis strains, as well as efficacy in a murine model of TB infection.
View MoreQINGDAO ON-BILLION INDUSTRAIL CO.,LTD
website:http://www.obn.com.cn
Contact:+86-15005320811 +86-532-80681989
Address:F35 Parkson Mansion No.44-60 Zhongshan Rd.
Tianjin Emulsion Science&Technology Development Co.,Ltd
Contact:13901380442
Address:Vake Garden New Town New Yi Bai Road Beichen District Tianjin,China
Jinzhou Jiutai Pharmaceutical Co.,Ltd
Contact:+86-0416-5179890
Address:No.41, Taianli, Taihe District, Jinzhou, Liaoning
Contact:+86 18616952870
Address:Area
Contact:86-791-86629460
Address:1-6F, 118 Xinzhou road, Nanchang, Jiangxi, China
Doi:10.1002/cmdc.201402186
(2014)Doi:10.1016/j.tetlet.2010.09.149
(2010)Doi:10.1016/j.crci.2013.02.001
(2014)Doi:10.1134/S1070428010100222
(2010)Doi:10.1021/ol102559f
(2011)Doi:10.1016/j.tet.2010.09.020
(2010)