Studies on Vazoactive Heterocyclic Compounds. : Preparation and Evaluation of the Hypotensive and Antiaggregating Activities of Phthalazinol Nitrates

SHIGERU ITO; YASUO KOMODA; SATOMI SEKIZAKI; HIROSHI AZUMA; MASAYUKI ISHIKAWA

doi:10.1248/cpb.36.2669

SHIGERU ITO, YASUO KOMODA, SATOMI SEKIZAKI, HIROSHI AZUMA, MASAYUKI ISHIKAWA

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Keywords: arachidonic acid

JOURNAL FREE ACCESS

1988 Volume 36 Issue 7 Pages 2669-2672

DOI https://doi.org/10.1248/cpb.36.2669

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Abstract

Phthalazinol (1) was converted to phthalazinol nitrate (2) and phthalazinol dinitrate (3) by treatment with fuming nitric acid and acetic anhydride. The structures were confirmed by spectral analyses. Introduction of the nitrogen dioxide moiety into the 4-hydroxymethyl group of 1 resulted in a potent hypotensive activity. Furthermore, the antiaggregating activities of 1 were remarkably enhanced by nitration of the 1-oxo and 4-hydroxymethyl groups.

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