Novel 2-Amino-1, 4-dihydropyridine Calcium Antagonists. I. Synthesis and Antihypertensive Effects of 2-Amino-1, 4-dihydropyridine Derivatives Having Nitroxyalkoxycarbonyl Groups at 3- and/or 5-Position

Takashi KOBAYASHI; Teruhiko INOUE; Zyunichiro KITA; Haruo YOSHIYA; Shigeyoshi NISHINO; Kiyoshi OIZUMI; Tomio KIMURA

doi:10.1248/cpb.43.788

Takashi KOBAYASHI, Teruhiko INOUE, Zyunichiro KITA, Haruo YOSHIYA, Shigeyoshi NISHINO, Kiyoshi OIZUMI, Tomio KIMURA

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Keywords: 1, 4-dihydropyridine, calcium antagonist, antihypertensive effect, spontaneously hypertensive rat, structure activity relationship

JOURNAL FREE ACCESS

1995 Volume 43 Issue 5 Pages 788-796

DOI https://doi.org/10.1248/cpb.43.788

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Abstract

Novel 2-amino-1, 4-dihydropyridine derivatives, which contain nitroxy-alkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their pharmaceutical effect was evaluated in spontaneously hypertensive rats. The structure-activity relationships are discussed in terms of potency, onset-rapidity, and duration of antihypertensive activity. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced on either side of an ester chain.

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