The optimization of pyridazinone series of glucan synthase inhibitors.
Rongze Kuang, Heping Wu, Pauline C Ting, Robert G Aslanian, Jianhua Cao, David W Kim, Joe F Lee, John Schwerdt, Gang Zhou, R Jason Herr, Andrew J Zych, Jinhai Yang, Sang Q Lam, David M Jenkins, Samuel A Sakwa, Samuel Wainhaus, Todd A Black, Anthony Cacciapuoti, Paul M McNicholas, Yiming Xu, Scott S Walker
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. rongze.kuang@merck.com
Bioorganic & medicinal chemistry letters 2012 Aug 15A 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. Copyright © 2012. Published by Elsevier Ltd.
Citation
Rongze Kuang, Heping Wu, Pauline C Ting, Robert G Aslanian, Jianhua Cao, David W Kim, Joe F Lee, John Schwerdt, Gang Zhou, R Jason Herr, Andrew J Zych, Jinhai Yang, Sang Q Lam, David M Jenkins, Samuel A Sakwa, Samuel Wainhaus, Todd A Black, Anthony Cacciapuoti, Paul M McNicholas, Yiming Xu, Scott S Walker. The optimization of pyridazinone series of glucan synthase inhibitors. Bioorganic & medicinal chemistry letters. 2012 Aug 15;22(16):5268-71
Mesh Tags
Substances
PMID: 22818082
View Full Text
