| Literature DB >> 19945877 |
Alexandre V Ivachtchenko1, Eugen B Frolov, Oleg D Mitkin, Sergei E Tkachenko, Ilya M Okun, Alex V Khvat.
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-pyrido[4,3-b]indole and its 5-phenethyl analog are the most potent blockers of 5-HT(7), 5-HT(6), 5-HT(2C), Adrenergic alpha(2) and H(1) 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-HT(7) receptors. Copyright 2009 Elsevier Ltd. All rights reserved.Entities:
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Year: 2009 PMID： 19945877 DOI： 10.1016/j.bmcl.2009.11.037
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823