Abstract
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.
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This study was supported financially by a 13115 project, No. 2007ZDKG-78, from Shaanxi Province, PR China.
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Guo, Zj., Zhou, K., Cao, Yx. et al. Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of lacidipine analogues. Med Chem Res 21, 1647–1651 (2012). https://doi.org/10.1007/s00044-011-9680-7
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DOI: https://doi.org/10.1007/s00044-011-9680-7