Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists,ACS Medicinal Chemistry Letters

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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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