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The optimization of pyridazinone series of glucan synthase inhibitors |
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| Authors: | 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 |
| Affiliation: | Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA. |
| Abstract: | 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. |
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