Chromenones as potent bradykinin B1 antagonists

…, SG Lehto, H Sun, FY Hsieh, C Xu, RT Fremeau…

Index: Bryan, Marian C.; Biswas, Kaustav; Peterkin, Tanya A.N.; Rzasa, Robert M.; Arik, Leyla; Lehto, Sonya G.; Sun, Hong; Hsieh, Feng-Yin; Xu, Cen; Fremeau, Robert T.; Allen, Jennifer R. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 619 - 622

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Citation Number: 5

Abstract

A series of fused 6, 6-bicyclic chromenones was investigated for activity against the bradykinin B1 receptor. SAR studies based on a pharmacophore model revealed compounds with high affinity for both human and rabbit B1. These compounds demonstrated favorable pharmacokinetic properties and 5-chlorochromenone 15 was efficacious in a carrageenan-induced mechanical hyperalgesia model for chronic pain.