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

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

  • Bioorg Med Chem Lett. 2013 Nov 15;23(22):6118-22. doi: 10.1016/j.bmcl.2013.09.016.
Alan Brown 1,  David Ellis,  David A Favor,  Tony Kirkup,  Wolfgang Klute,  Malcolm MacKenny,  Gordon McMurray,  Adam Stennett
Affiliations

Affiliation

  • 1 Worldwide Medicinal Chemistry, Pfizer Neusentis, Granta Park, Great Abington, Cambridge CB21 6GS, UK. Electronic address: Alan.D.Brown@pfizer.com.
PMID: 24080460 DOI: 10.1016/j.bmcl.2013.09.016
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.

Keywords

1,3-Diamino cyclohexane; Lead hopping; Library design; Multi-dimensional scaling; TRPM8.

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