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Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2017-09-06 00:00:00 , DOI: 10.1021/acsmedchemlett.7b00315
Nicholas Kindon 1 , Glen Andrews 1 , Andrew Baxter 1 , David Cheshire 1 , Paul Hemsley 1 , Timothy Johnson 1 , Yu-Zhen Liu 1 , Dermot McGinnity 1 , Mark McHale 1 , Antonio Mete 1 , James Reuberson 1 , Bryan Roberts 1 , John Steele 1, 2 , Barry Teobald 1 , John Unitt 1 , Deborah Vaughan 1 , Iain Walters 1 , Michael J. Stocks 1
Affiliation  

N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high-throughput screen (HTS) of a subset of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excellent starting point for a CCR4 receptor antagonist program and enabled the rapid progression through the Lead Identification and Lead Optimization phases resulting in the discovery of two bioavailable CCR4 receptor antagonist candidate drugs.

中文翻译:

发现两种有效的可生物利用的CCR4受体拮抗剂AZD-2098和AZD-1678

在阿斯利康化合物库的一个子集的CCR4受体拮抗剂高通量筛选(HTS)中,N-(5-溴-3-甲氧基吡嗪-2-基)-5-氯噻吩-2-磺酰胺1被鉴定为命中。作为具有铅样特征的命中分子,它是CCR4受体拮抗剂计划的绝佳起点,并且能够通过“铅鉴定”和“铅优化”阶段快速发展,从而导致发现了两种可生物利用的CCR4受体拮抗剂候选药物。
更新日期:2017-09-06
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