866764-34-3Relevant academic research and scientific papers
Synthesis of new sulfonamide derivatives of thiazolo[3,2-a]quinazolin-5-one
Shlenev,Filimonov,Tarasov,Danilova,Agat’ev
, p. 69 - 75 (2016)
A general procedure has been proposed for the synthesis of thiazolo[3,2-a]quinazolin-5-one derivatives containing a sulfonamide group on C7via intramolecular nucleophilic substitution of halogen in 2-halo-5-sulfamoyl-N-(1,3-thiazol-2-yl)benzami
Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639
Zhang, Qingwei,Xia, Zhiren,Joshi, Shailen,Scott, Victoria E.,Jarvis, Michael F.
supporting information, p. 641 - 644 (2015/06/30)
The discovery of a novel peripherally acting and selective Cav3.2 T-type calcium channel blocker, ABT-639, is described. HTS hits 1 and 2, which have poor metabolic stability, were optimized to obtain 4, which has improved stability and oral bi
Structure-activity relationships of novel potent MurF inhibitors
Gu, Yu Gui,Florjancic, Alan S.,Clark, Richard F.,Zhang, Tianyuan,Cooper, Curt S.,Anderson, David D.,Lerner, Claude G.,McCall, J. Owen,Cai, Yingna,Black-Schaefer, Candace L.,Stamper, Geoffrey F.,Hajduk, Philip J.,Beutel, Bruce A.
, p. 267 - 270 (2007/10/03)
A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC 50=22～70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers.
