The optimization of pyridazinone series of glucan synthase inhibitors

Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
Bioorganic & medicinal chemistry letters (Impact Factor: 2.42). 07/2012; 22(16):5268-71. DOI: 10.1016/j.bmcl.2012.06.091
Source: PubMed


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.

30 Reads