Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles |
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Authors: | Alexandre V Ivachtchenko Eugen B Frolov Oleg D Mitkin Sergei E Tkachenko Ilya M Okun Alex V Khvat |
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Institution: | 1. Department of Organic Chemistry, Chemical Diversity Research Institute, 114401 Khimki, Moscow Reg, Russia;2. ChemDiv, Inc., 6605 Nancy Ridge Drive, San Diego, CA 92121, USA |
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Abstract: | 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-pyrido4,3-b]indole 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. |
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