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

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 synthesised with the least degree of similarity to the lead structure.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Brown A,Ellis D,Favor DA,Kirkup T,Klute W,MacKenny M,McMurray G,Stennett A

doi

10.1016/j.bmcl.2013.09.016

subject

Has Abstract

pub_date

2013-11-15 00:00:00

pages

6118-22

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)01079-2

journal_volume

23

pub_type

杂志文章

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