发现一类新型的葡萄糖神经酰胺合酶抑制剂。
Discovery of a new class of glucosylceramide synthase inhibitors.
机构信息
Exelixis, 210 E. Grand Avenue, South San Francisco, CA 94005, USA.
出版信息
Bioorg Med Chem Lett. 2011 Nov 15;21(22):6773-7. doi: 10.1016/j.bmcl.2011.09.037. Epub 2011 Sep 17.
PMID:21974949
Abstract
A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.
摘要
本文描述了一系列新型强效的葡萄糖神经酰胺合酶抑制剂。通过对生化和细胞效力以及 ADME 性质的优化，得到了化合物 23c。在给小鼠口服后，它在广泛的组织中都有分布。因此，23c 可能成为另一种有用的工具化合物，用于研究体外和体内 GCS 抑制的作用。
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