Serendipity in drug-discovery: A new series of 2-(benzyloxy) benzamides as TRPM8 antagonists

…, W Klute, M MacKenny, G McMurray, A Stennett

文献索引：Brown, Alan; Ellis, David; Favor, David A.; Kirkup, Tony; Klute, Wolfgang; MacKenny, Malcolm; McMurray, Gordon; Stennett, Adam Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 22 p. 6118 - 6122

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被引用次数: 6

摘要

Abstract A new series of 2-(benzyloxy) benzamides are presented that are potent functional antagonists of TRPM8 and possess improved LipE and LE compared to the original lead. They were discovered through a series of compound libraries and we present a powerful visualization method for the chemical space explored with each library. Remarkably this new series originated from the highest risk design strategy where compounds were ...