新型强效 CRTH2 拮抗剂的发现。
Discovery of novel and potent CRTH2 antagonists.
机构信息
Chemistry Research Labs, Drug Discovery Research, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1194-7. doi: 10.1016/j.bmcl.2011.11.079. Epub 2011 Nov 28.
PMID:22178554
Abstract
High throughput screening of our chemical library for CRTH2 antagonists provided a lead compound 1a. Initial optimization of the lead led to the discovery of a novel, potent and orally bioavailable CRTH2 antagonist 17.
摘要
高通量筛选我们的化学文库以寻找 CRTH2 拮抗剂，得到了先导化合物 1a。对该先导化合物的初步优化导致发现了一种新型、有效且可口服生物利用的 CRTH2 拮抗剂 17。
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