1062072-35-8Relevant academic research and scientific papers
The optimization of pyridazinone series of glucan synthase inhibitors
Kuang, Rongze,Wu, Heping,Ting, Pauline C.,Aslanian, Robert G.,Cao, Jianhua,Kim, David W.,Lee, Joe F.,Schwerdt, John,Zhou, Gang,Jason Herr,Zych, Andrew J.,Yang, Jinhai,Lam, Sang Q.,Jenkins, David M.,Sakwa, Samuel A.,Wainhaus, Samuel,Black, Todd A.,Cacciapuoti, Anthony,McNicholas, Paul M.,Xu, Yiming,Walker, Scott S.
scheme or table, p. 5268 - 5271 (2012/09/07)
A detailed structure-activity relationship study of a novel series of pyridazine-based small molecule glucan synthase inhibitors is described. The optimization of the PK profile of this series led to the discovery of compound 11g, which demonstrated in vivo potency ip in a lethal fungal infection model.
The synthesis and structure-activity relationship of pyridazinones as glucan synthase inhibitors
Ting, Pauline C.,Kuang, Rongze,Wu, Heping,Aslanian, Robert G.,Cao, Jianhua,Kim, David W.,Lee, Joe F.,Schwerdt, John,Zhou, Gang,Wainhaus, Samuel,Black, Todd A.,Cacciapuoti, Anthony,McNicholas, Paul M.,Xu, Yiming,Walker, Scott S.
scheme or table, p. 1819 - 1822 (2011/05/05)
A structure-activity relationship study of the lead 5-[4-(benzylsulfonyl) piperazin-1-yl]-4-morpholino-2-phenyl-pyridazin-3(2H)-one 1 has resulted in the identification of 2-(3,5-difluorophenyl)-4-(3-fluorocyclopentyloxy)-5-[4- (isopropylsulfonyl)piperazin-1-yl]-pyridazin-3(2H)-one 11c as a β-1,3-glucan synthase inhibitor. Compound 11c exhibited significant efficacy in an in vivo mouse model of Candida glabrata infection.
