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

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

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 pr...

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Veröffentlicht in:ACS medicinal chemistry letters 2017-09, Vol.8 (9), p.981-986
Hauptverfasser: 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
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Sprache:eng
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/acsmedchemlett.7b00315