2-Ethynylbenzenealkanamines. A new class of calcium entry blockers.

Autor: Carson JR; McNeil Pharmaceutical, Spring House, Pennsylvania 19477-0776., Almond HR, Brannan MD, Carmosin RJ, Flaim SF, Gill A, Gleason MM, Keely SL, Ludovici DW, Pitis PM, et. al.
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1988 Mar; Vol. 31 (3), pp. 630-6.
DOI: 10.1021/jm00398a023
Abstrakt: A series of 2-(aryl- or alkylethynyl)benzenealkanamines were synthesized. They exhibit antihypertensive activity in spontaneously hypertensive rats and coronary vasodilator activity with minimal negative inotropic activity in the "Langendorff" guinea pig heart in vitro. They have been shown to exert their activity by inhibition of Ca2+ influx across cell membranes. Optimal activity is found among the N-(arylethyl)-5-methoxy-alpha-methyl-2-(phenylethynyl)ben zeneethanamines and -propanamines.
Databáze: MEDLINE