1208230-75-4Relevant academic research and scientific papers
Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles
Ivachtchenko, Alexandre V.,Frolov, Eugen B.,Mitkin, Oleg D.,Tkachenko, Sergei E.,Okun, Ilya M.,Khvat, Alex V.
supporting information; experimental part, p. 78 - 82 (2010/04/02)
Syntheses, biological evaluation, and structure-activity relationships for a series of novel 5-styryl and 5-phenethyl analogs of dimebolin are disclosed. The novel derivatives and dimebolin share a broad spectrum of activities against therapeutically relevant targets. Among all synthesized derivatives, 2,8-dimethyl-5-[(Z)-2-phenylvinyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]in dole and its 5-phenethyl analog are the most potent blockers of 5-HT7, 5-HT6, 5-HT2C, Adrenergic α2 and H1 receptors. The general affinity rank order towards the studied receptors was Z-3(2) > 4(2) ≥ 4(3) ? dimebolin, all of them having highest affinities to 5-HT7 receptors.
