环丙基氨基酸酰胺作为2,3-二氨基吡啶的药效团替代物。应用于新型缓激肽B1受体拮抗剂的设计。
Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.
作者信息
Wood Michael R, Schirripa Kathy M, Kim June J, Wan Bang-Lin, Murphy Kathy L, Ransom Richard W, Chang Raymond S L, Tang Cuyue, Prueksaritanont Thomayant, Detwiler Theodore J, Hettrick Lisa A, Landis Elizabeth R, Leonard Yvonne M, Krueger Julie A, Lewis Sidney D, Pettibone Douglas J, Freidinger Roger M, Bock Mark G
出版信息
J Med Chem. 2006 Feb 23;49(4):1231-4. doi: 10.1021/jm0511280.
PMID:16480259
Abstract
Antagonism of the bradykinin B1 receptor represents a potential treatment for chronic pain and inflammation. Novel antagonists were designed that display low-nanomolar affinity for the human bradykinin B1 receptor and good bioavailability in the rat.
摘要
缓激肽B1受体拮抗剂是慢性疼痛和炎症的一种潜在治疗方法。设计了对人缓激肽B1受体具有低纳摩尔亲和力且在大鼠中具有良好生物利用度的新型拮抗剂。
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