一类新型口服活性非肽类内皮素-A受体拮抗剂的发现与优化
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
作者信息
Riechers H, Albrecht H P, Amberg W, Baumann E, Bernard H, Böhm H J, Klinge D, Kling A, Müller S, Raschack M, Unger L, Walker N, Wernet W
机构信息
Hauptlaboratorium, BASF AG, Ludwigshafen, Germany.
出版信息
J Med Chem. 1996 May 24;39(11):2123-8. doi: 10.1021/jm960274q.
PMID:8667356
Abstract
A novel class of endothelin-A receptor ligands was discovered by high-throughput screening. Lead structure optimization led to highly potent antagonists which can be synthesized in a short sequence. The compounds are endothelin-A-selective, are orally available, and show a long duration of action.
摘要
通过高通量筛选发现了一类新型的内皮素-A受体配体。先导结构优化产生了高效拮抗剂，这些拮抗剂可通过短序列合成。这些化合物对内皮素-A具有选择性，口服可用，且作用持续时间长。
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