吡嗪酮类葡聚糖合成酶抑制剂的优化。
The optimization of pyridazinone series of glucan synthase inhibitors.
机构信息
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2012 Aug 15;22(16):5268-71. doi: 10.1016/j.bmcl.2012.06.091. Epub 2012 Jul 4.
PMID:22818082
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.
摘要
本文详细描述了一系列新型基于哒嗪的小分子葡聚糖合酶抑制剂的构效关系研究。该系列化合物的 PK 特性得到了优化，发现了化合物 11g，在致命真菌感染模型中，它具有良好的体内活性。
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