Synthesis, antiplatelet aggregation activity, and molecular modeling study of novel substituted-piperazine analogues

Autor:	Hussein I. El-Subbagh, Abdel-Galil M. Abdel-Gader, Laila A. Abou-Zeid, Mohamed A. Al-Omar, Khairia M. Youssef, Ali S. Al-Tuwaijri, Nadia G. Haress
Rok vydání:	2010
Předmět:	Piperazine chemistry.chemical_compound chemistry Platelet aggregation Molecular model Hydrobromide Stereochemistry Organic Chemistry Lipophilicity Pharmacology toxicology Nipecotic acid Structure–activity relationship General Pharmacology Toxicology and Pharmaceutics
Zdroj:	Medicinal Chemistry Research. 20:898-911
ISSN:	1554-8120 1054-2523
DOI:	10.1007/s00044-010-9411-5
Popis:	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 μM.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f229725511e0f3b604eb30f82675f368 https://doi.org/10.1007/s00044-010-9411-5 Zobrazit plný text záznamu Full text from SpringerLink