@SYNTHESIS AND SMOOTH MUSCLE CALCIUM CHANNEL ANTAGONIST EFFECT OF ALKYL, AMINOALKYL 1,4-DIHYDRO-2,6-DIMETHYL-4-NITROIMIDAZOLE-3,5 PYRIDINE DICARBOXYLATES

摘要: The discovery that 1,4-dihydropyridine (DHP) class of calcium channel antagonist inhibits the Ca+² influx represented a major therapeutic advance in treatment cardiovascular diseases such as hypertension, angina pectoris and other spastic smooth muscle disorders. A novel flunarizine containing arylpiperazinyl moiety has recently been reported. It was therefore interest to determine effect selected C-3 substituents contained amino alkyl arylpiperazine, conjunction with C-4 1-methyl-5-nitro-2-imidazolyl on activity. unsymmetrical analogues were prepared by procedure reported Meyer which 1-methyl-5-nitro-imidazol-2-carboxaldehyde reacted acetoacetic esters 3-aminocrotonate. In vitro activities determined use high K+ contraction guinea pig ileal longitudinal muscle. All compounds exhibited comparable activity (IC50=10^-9 10^-11 M) against reference drug nifedipine (IC50=2.75±0.36 x 10^-10 M).