前往化源商城

Journal of medicinal and pharmaceutical chemistry 2008-07-10

Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships.

Rohan J Kumar, Mary Chebib, David E Hibbs, Hye-Lim Kim, Graham A R Johnston, Noeris K Salam, Jane R Hanrahan

文献索引:J. Med. Chem. 51 , 3825-40, (2008)

全文:HTML全文

摘要

Gamma-aminobutyric acid (GABA) analogues based on 4-amino-cyclopent-1-enyl phosphinic acid ( 34- 42) and 3-aminocyclobutane phosphinic acids ( 51, 52, 56, 57) were investigated in order to obtain selective homomeric rho 1 GABA C receptor antagonists. The effect of the stereochemistry and phosphinic acid substituent of these compounds on potency and selectivity within the GABA receptor subtypes was investigated. Compounds of high potency at GABA C rho 1 receptors ( 36, K B = 0.78 microM) and selectivity greater than 100 times ( 41, K B = 4.97 microM) were obtained. The data obtained was analyzed along with the known set of GABA C rho 1 receptor-ligands, leading to the development of a pharmacophore model for this receptor, which can be used for in silico screening.

相关化合物

结构式 名称/CAS号 全部文献
4-氨基丁酸 结构式 4-氨基丁酸
CAS:56-12-2
5-氨基戊酸 结构式 5-氨基戊酸
CAS:660-88-8