Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of lacidipine analogues

Six analogues of lacidipine, ( E )-diethyl 4-(2-(3-amino)-3-oxoprop-1-enyl)phenyl-2, 6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates (compounds 1 – 6 ), were synthesized and their antihypertensive effects in spontaneously hypertensive rats were evaluated by ig administration. Amongst the tested compounds, compound 5 exhibited the highest antihypertensive effect. The lasting time and potency of compound 5 showed a dose-dependent manner. The results suggested that N - tert -butyl acrylamide moiety at 2′-position of 4-phenyl in the structure of analogues of lacidipine is necessary to keep antihypertensive effects.