5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation

Autor:	Sergey D. Varfolomeev, E. I. Sinauridze, V. I. Shvets, O. V. Demina, A. A. Khodonov
Rok vydání:	2014
Předmět:	Nitrile biology Stereochemistry General Chemistry Cycloaddition chemistry.chemical_compound chemistry biology.protein Platelet Arachidonic acid Cyclooxygenase Thromboxane-A synthase Isoxazole Discovery and development of direct thrombin inhibitors
Zdroj:	Russian Chemical Bulletin. 63:2092-2113
ISSN:	1573-9171 1066-5285
Popis:	A series of 5-substituted 3-pyridylisoxazoles were synthesized using [3+2] cycloaddition of nitrile oxides to alkynes with variation of substituents at position 5 of the isoxazole ring without additional synthetic stages and with retention of 2-pyridyl-, 3-pyridyl, and 4-pyridyl substituents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential antiaggregatory agents showing in vitro activity in the concentration range from 1•10−6 mol L−1 to 1•10−4 mol L−1 toward the human platelet rich blood plasma with arachidonic acid being used as the inductor of aggregation. These compounds do not act as cyclooxygenase or thromboxane synthase inhibitors, nor as thrombin inhibitors.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::059bcc8475f5bfa4bf0aa68ade650da9 https://doi.org/10.1007/s11172-014-0707-3 Zobrazit plný text záznamu Full text from SpringerLink