Studies on antiallergy agents. III. Synthesis of 2-anilino-1,6-dihydro-6-oxo-5-pyrimidinecarboxylic acids and related compounds

Chem Pharm Bull (Tokyo). 1989 Jul;37(7):1780-7. doi: 10.1248/cpb.37.1780.

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.

MeSH terms

  • Aniline Compounds / chemical synthesis*
  • Aniline Compounds / pharmacology
  • Aniline Compounds / toxicity
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Histamine H1 Antagonists / chemical synthesis*
  • Histamine H1 Antagonists / pharmacology
  • Histamine H1 Antagonists / toxicity
  • Hypersensitivity / drug therapy*
  • Male
  • Mice
  • Mice, Inbred Strains
  • Passive Cutaneous Anaphylaxis / drug effects
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Pyrimidines / toxicity
  • Rats
  • Rats, Inbred Strains

Substances

  • Aniline Compounds
  • Histamine H1 Antagonists
  • Pyrimidines