Synthesis and biological activity of 5-styryl and 5-phenethyl-substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles

Bioorganic & Medicinal Chemistry Letters
Alexandre V IvachtchenkoAlex 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.

Citations

Sep 23, 2014·European Journal of Medicinal Chemistry·Robert OttoChristoph Enzensperger
May 28, 2016·Journal of Alzheimer's Disease : JAD·Alexandre V IvachtchenkoIlya Okun
Jan 28, 2017·Accounts of Chemical Research·Monika PatelAkhilesh K Verma
Mar 17, 2015·ChemMedChem·Dawid WarszyckiAndrzej J Bojarski
Aug 30, 2011·CNS Drugs·Werner J Geldenhuys, Cornelis J Van der Schyf
Jun 26, 2014·Angewandte Chemie·Alexandre HentzRobert H Dodd
May 26, 2018·The Journal of Organic Chemistry·Mingwei ZhouXuhong Qian

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