Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists

作者:Kindon Nicholas; Andrews Glen; Baxter Andrew; Cheshire David; Hemsley Paul; Johnson Timothy; Liu Yu Zhen; McGinnity Dermot; McHale Mark; Mete Antonio; Reuberson James; Roberts Bryan; Steele John; Teobald Barry; Unitt John; Vaughan Deborah; Walters Iain; Stocks Michael J*
来源:ACS Medicinal Chemistry Letters, 2017, 8(9): 981-986.
DOI:10.1021/acsmedchemlett.7b003115

摘要

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.

  • 出版日期2017-9

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