期刊
MEDICINAL CHEMISTRY RESEARCH
卷 20, 期 7, 页码 898-911出版社
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-010-9411-5
关键词
Synthesis; Piperazine analogues; Antiplatelet aggregation; Molecular modeling studies
资金
- King Abdulaziz City for Science and Technology [AR-25-50]
New carbamoylpyridine and carbamoylpiperidine analogues containing nipecotic acid scaffold were designed, synthesized, and evaluated for their platelet aggregation inhibitory activity. Molecular modeling investigation was performed and the impact of lipophilicity on activity was also discussed. Structure activity relationship among this series was obtained. N (1)-[1-(4-bromobenzyl)-3-piperidino-carbonyl]-N (4)-(2-chlorophenyl)-piperazine hydrobromide (20), and 1,4-bis-[3-[N (4)-(2-chlorophenyl)-N (1)-(piperazino-carbonyl)]-piperidin-1-yl-methyl]-benzene dibromide (30) are the most active antiplatelet aggregating compounds in this study, both at concentration of 0.06 mu M.
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