NDLI: Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones

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Synthesis and dual D2 and 5-HT1A receptor binding affinities of 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones

Content Provider	Taylor & Francis Online
Author	Ullah, Nisar
Abstract	A series of new 5-piperidinyl and 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones have been synthesized and evaluated for dual D2 and 5-HT1A receptor binding affinities. The synthesized ligands are structurally related to bifeprunox, a potential atypical antipsychotic, having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. The Suzuki–Miyaura reaction of cyclic vinyl boronate with appropriate aryl halide yielded arylpiperidine, which was eventually transformed to piperidinyl-1H-benzo[d]imidazol-2(3H)-one. The reductive amination of the latter with appropriate biarylaldehdyes rendered the synthesis of 5-piperidinyl-1H-benzo[d]imidazol-2(3H)-ones. Likewise, the Buchwald–Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halide and subsequent removal of the boc group rendered arylpiperazine. The reductive amination of the latter with appropriate biarylaldehdyes accomplished the synthesis of 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones. The structure–activity relationship studies showed that cyclopentenylpyridine and cyclopentenylbenzyl groups contribute significantly to the dual D2 and 5-HT1A receptor binding affinities of these compounds.
Starting Page	281
Ending Page	291
Page Count	11
File Format	PDF HTM / HTML
ISSN	14756366 14756374
DOI	10.3109/14756366.2013.776556
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume Number	29
Issue Number	2
Language	English
Publisher	Taylor & Francis
Publisher Date	2014-03-12
Access Restriction	Open
Subject Keyword	5-HT1A receptor 5-piperidinyl-1H-benzo[d]imidazol-2(3H)-ones 5-piperazinyl-1H-benzo[d]imidazol-2(3H)-ones D2 receptor Schizophrenia
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Medicine Pharmacology

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