Channelpedia

PubMed 24080460


Referenced in Channelpedia wiki pages of: none

Automatically associated channels: TRP , TRPM , TRPM8



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

Authors: Alan Brown, David Ellis, David A Favor, Tony Kirkup, Wolfgang Klute, Malcolm MacKenny, Gordon McMurray, Adam Stennett

Journal, date & volume: Bioorg. Med. Chem. Lett., 2013 Nov 15 , 23, 6118-22

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/24080460


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.