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Bioorg Med Chem Lett. 2012 Aug 15;22(16):5268-71. doi: 10.1016/j.bmcl.2012.06.091. Epub 2012 Jul 4.

The optimization of pyridazinone series of glucan synthase inhibitors.

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  • 1Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.


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.

Copyright © 2012. Published by Elsevier Ltd.

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