Studies on Antiallergy Agents. III. Synthesis of 2-Anilino-1, 6-dihydro-6-oxo-5-pyrimidinecarboxylic Acids and Related Compounds

Kohji OZEKI; Teru ICHIKAWA; Hiroyuki TAKEHARA; Kenjiro TANIMURA; Makoto SATO; Hideya YAGINUMA

doi:10.1248/cpb.37.1780

Kohji OZEKI, Teru ICHIKAWA, Hiroyuki TAKEHARA, Kenjiro TANIMURA, Makoto SATO, Hideya YAGINUMA

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Keywords: antiallergy agent, intraperitoneal activity, oral activity, 1, 6-dihydro-6-oxo-5-pyrimidinecarboxylic acid, phenyl-guanidine, structure-activity relationship

JOURNAL FREE ACCESS

1989 Volume 37 Issue 7 Pages 1780-1787

DOI https://doi.org/10.1248/cpb.37.1780

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Abstract

A series of 2-anilino-1, 6-dihydro-6-oxo-5-pyrimidinecarboxylic acids with various substituents was synthesized and evaluated in the rat passive cutaneous anaphylaxis test for antiallergic activity. High activity by intraperitoneal and oral administrations was observed for the 3-trifluoromethyl and 2-alkoxyanilino derivatives (64, 79, 81, 82 and 85).Structure-activity relationships are discussed.

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