, Volume 20, Issue 8, pp 1325-1330
Date: 28 Oct 2010

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

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The antihypertensive activity of nitrendipine analogues can be improved by properly lengthening its alkyl chain in 3- or 5-position. Nitrendipine and its seven analogues were synthesized, and their antihypertensive activities in spontaneously hypertensive rats (SHR) were evaluated by ig administration. It was found that 5-n-heptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate [(±)-5] exhibited the strongest antihypertensive effect amongst eight compounds. (+)-5-n-heptyl 3-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate [(+)-5] was also prepared. Antihypertensive activities of (±)-5 and (+)-5 in SHR were compared. The results showed that (±)-5 and (+)-5 had a higher potency than nitrendipine, and (+)-isomer was 1.79-fold the raceme at a dose of 2 mg/kg.