molecules of the month

compound 59

TRPM8 blocker for ocular administration

effective w/ ocular admin. in animal model

cell-based screen. and opt. of thiazoles series

Journal of Medicinal Chemistry

Dompé Farmaceutici S.p.A

Chemical structure of compound 59 Dompé Farmaceutici TRPM8 blocker
1 min read

12. The Dompé Farmaceutici TRPM8 blocker, compound 59 is a potent (IC50 = 11 nM) compound for painful ocular conditions, with ocular efficacy in a preclinical behavioral model. TRPM8 is a cation channel which is the predominant in mammalian cold thermosensor and it is activated by well-known molecules like menthol, eucalyptol, and geraniol. The starting points were previous drug candidates tetrazole DFL23448 and ketone DFL23693. The molecule possesses an unusual hydroxythiazole which was found to be critical for activity. An unusual N-alkoxy amide was also employed, with surprisingly sharp SAR. The compound shows rapid activity in a preclinical model (15 min post dose) and is an rare case study for ocular drug discovery.

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