期刊
MEDICINAL CHEMISTRY
卷 10, 期 5, 页码 484-496出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/15734064113096660046
关键词
D-2 receptor; 5-HT1A receptor; 7-Piperazinyl and piperidinyl-3,4-dihydroquinazolin-2(1H)-ones; Schizophrenia; Structure-activity relationship
资金
- KACST Project [AR-28-38]
A series of new 7-piperazinyl and 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones has been synthesized. The described compounds are structurally related to adoprazine, a potential atypical antipsychotic bearing potent D-2 receptor antagonist and 5-HT1A receptor agonist properties. Suitably modified aryl bromides were prepared and condensed with tert-butyl piperazine-1-carboxylate to afford the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Likewise Suzuki-Miyaura cross-coupling reaction of cyclic vinyl boronate with appropriate aryl bromides rendered piperidinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the piperazinyl and piperidinyl-3,4-dihydroquinazolin- 2(1H)-ones with suitably designed biarylaldehydes accomplished the synthesis of these title compounds. The described compounds were screened for D-2 and 5-HT1A receptors binding affinities. The structure-activity relationship studies revealed that cyclopentenylpyridine and cyclopentenylbenzyl groups contribute significantly to the dual D-2 and 5-HT1A receptor binding affinities of these compounds.
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