Novel 1, 4-Dihydropyridine Calcium Antagonists. I. : Synthesis and Hypotensive Activity of 4-(Substituted Pyridyl)-1, 4-dihydropyridine Derivatives

抄録

A series of 4-(substituted pyridyl)-1, 4-dihydropyridine derivatives were synthesized and their hypotensive effects examined. Several compounds, 2-(N-benzyl-N-methylamino)ethyl methyl 1, 4-dihydro-2, 6-dimethyl-4-(3-nitro-2-pyridyl)-3, 5-pyridinedicarboxylate (2b), its 4-(4-nitro-2-pyridyl) analogue (2g), 4-(3-trifluoromethyl-2-pyridyl) analogue (2c), 4-(2-trifluoromethyl-3-pyridyl) analogue (3e), 4-(4-cyano-2-pyridyl) analogue (2e), 4-(2-cyano-3-pyridyl) analogue (3d), and 4-(6-bromo-2-pyridyl) analogue (2i), were found to have a hypotensive activity parallel to that of nicardipine; 2c and 3e, in particular, had approximately twice the duration of nicardipine, and 2e had the most potent hypotensive activity of all the derivatives synthesized.