Chromenones as potent bradykinin B1 antagonists
2012
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.
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.
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