Quinolizidinyl-benzimidazoles as platelet-antiaggregating agents.

作者: Iana Vazzana , Emanuela Terranova , Bruno Tasso , Michele Tonelli , Antonietta Piana

DOI: 10.1002/CBDV.200890068

关键词:

摘要: Two series of (+/-)-2-phenyl-1-(quinolizidin-1 alpha-yl)benzimidazoles, 12A-26A, and beta-yl)benzimidazoles, 12B-26B, were prepared tested for the inhibition human platelets aggregation induced by ADP, collagen, adrenaline. All epimers A, i.e., devoid any activity against three agonists, while B, exhibited different degrees activity, though practically confined ADP-induced aggregation. The best compounds 19B, 24B, 26B, which inhibited 69-67% at 260 microM 40-29% 65 concentration ADP (2 microM)-induced observed agonist spatial structure selectivity warrant further investigations this kind benzimidazole derivatives.

参考文章(20)
Anna Sparatore, Nicoletta Basilico, Silvia Parapini, Sergio Romeo, Federica Novelli, Fabio Sparatore, Donatella Taramelli, 4-amino-quinoline ouinolizidinyl-and quinolizidinylalkyl-derivatives with antimalarial activity Bioorganic & Medicinal Chemistry. ,vol. 13, pp. 5338- 5345 ,(2004) , 10.1016/J.BMC.2005.06.047
Shaker A. Mousa, Mark S Forsythe, Jeff M Bozarth, Thomas M. Reilly, Effect of Single Oral Dose of Aspirin on Human Platelet Functions and Plasma Plasminogen Activator Inhibitor-1 Cardiology. ,vol. 83, pp. 367- 373 ,(1993) , 10.1159/000175993
Deepak L. Bhatt, Eric J. Topol, Scientific and therapeutic advances in antiplatelet therapy. Nature Reviews Drug Discovery. ,vol. 2, pp. 15- 28 ,(2003) , 10.1038/NRD985
Paolo Gresele, Giancarlo Agnelli, Novel approaches to the treatment of thrombosis. Trends in Pharmacological Sciences. ,vol. 23, pp. 25- 32 ,(2002) , 10.1016/S0165-6147(00)01885-X
Federica Novelli, Bruno Tasso, Fabio Sparatore, Synthesis and pharmacological evaluation of some thiolupinine derivatives Farmaco. ,vol. 54, pp. 354- 358 ,(1999) , 10.1016/S0014-827X(99)00041-5
N. C. Franklin, H. Feltkamp, Conformational Analysis of Cyclohexane Derivatives by Nuclear Magnetic Resonance Spectroscopy Angewandte Chemie. ,vol. 4, pp. 774- 783 ,(1965) , 10.1002/ANIE.196507741
Michael S Hadley, Frank D King, Brian McRitchie, David H Turner, Eric A Watts, None, Substituted benzamides with conformationally restricted side chains. 1. Quinolizidine derivatives as selective gastric prokinetic agents Journal of Medicinal Chemistry. ,vol. 28, pp. 1843- 1847 ,(1985) , 10.1021/JM00150A015