Anti-inflammatory aryl para-aminomethylbenzoate derivatives

Abstract

Aryl esters of 4-aminomethylbenzoic acid and their use as tryptase inhibitors are claimed. The compounds are potent inhibitors of the serine protease tryptase with nanomolar potencies. They display a limited degree of selectivity relative to trypsin and variable stability to plasma esterases. Substitution of the aryl group, by polar substituents, markedly improves plasma stability. These compounds are the first evidence from Proteus Molecular Design (now Protherics) of their approach to designing tryptase inhibitors.

• asthma
• benzoate
• benzylamine
• serine protease
• trypsin
• tryptase