潜在的抗焦虑药。第4部分：具有高γ-氨基丁酸A受体亲和力的新型口服活性N(5)-取代吡啶并[1,2-a]苯并咪唑类化合物
Potential anxiolytic agents. Part 4: novel orally-active N(5)-substituted pyrido[1,2-a]benzimidazoles with high GABA-A receptor affinity.
作者信息
Jordan Alfonzo D, Vaidya Anil H, Rosenthal Daniel I, Dubinsky Barry, Kordik Cheryl P, Sanfilippo Pauline J, Wu Wu-Nan, Reitz Allen B
机构信息
Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA.
出版信息
Bioorg Med Chem Lett. 2002 Sep 2;12(17):2381-6. doi: 10.1016/s0960-894x(02)00463-8.
A series of pyrido[1,2-a]benzimidazoles (PBIs) with substitution on the N(5)-nitrogen has been synthesized and found to possess high affinity for the benzodiazepine (BZD) site on the GABA-A receptor. The compounds evaluated include those bearing a heteroalkyl group and heterocyclic rings. The most promising of these compounds is ethoxymethyl analogue 24, which has an IC(50) of 0.1 nM for the BZD site on the GABA-A receptor and has been advanced to human clinical trials.
一系列在N(5)-氮上有取代基的吡啶并[1,2-a]苯并咪唑（PBIs）已被合成，并发现它们对GABA-A受体上的苯二氮䓬（BZD）位点具有高亲和力。所评估的化合物包括带有杂烷基和杂环的那些。这些化合物中最有前景的是乙氧基甲基类似物24，它对GABA-A受体上的BZD位点的IC(50)为0.1 nM，并且已进入人体临床试验阶段。
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