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.
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.
p. 619 - 622
(2012/02/04)
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