强效缓激肽B1受体拮抗剂：4-取代苯基环己烷。

Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

作者信息

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

机构信息

Department of Medicinal Chemistry, West Point, PA 19486, USA.

出版信息

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3006-9. doi: 10.1016/j.bmcl.2007.03.059. Epub 2007 Mar 21.

DOI:10.1016/j.bmcl.2007.03.059

PMID:17428657

Abstract

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.

摘要

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。