Su Dai-Shi, Lim John L, Markowitz M Kristine, Wan Bang-Lin, Murphy Kathy L, Reiss Duane R, Harrell C Meacham, O'Malley Stacy S, Ransom Rick W, Chang Raymond S L, Pettibone Douglas J, Tang Cuyue, Prueksaritanont Thomayant, Freidinger Roger M, Bock Mark G
Department of Medicinal Chemistry, West Point, PA 19486, USA.
Bioorg Med Chem Lett. 2007 Jun 1;17(11):3006-9. doi: 10.1016/j.bmcl.2007.03.059. Epub 2007 Mar 21.
Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B(1) receptor antagonists.
选择性缓激肽（BK）B(1)受体拮抗剂在动物模型中已显示出具有抗伤害感受作用，可能成为治疗疼痛和炎症的新型治疗药物。对先导化合物1的联苯部分的构效关系进行阐释，得到了一类强效的新型BK B(1)受体拮抗剂结构。
