Studies on antiulcer drugs. V. Synthesis and antiulcer activity of aralkylbenzazoles

Chem Pharm Bull (Tokyo). 1992 Aug;40(8):2062-74. doi: 10.1248/cpb.40.2062.

Abstract

A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagonist activity in contrast to imidazo[1,2-a]pyridine analogues (I). On antiulcer assay, however, some pyridine derivatives (II) exerted higher activity than the reference compounds, sofalcone, sucralfate and cimetidine. The structure-activity relationships of these compounds are discussed.

MeSH terms

  • Animals
  • Anti-Ulcer Agents / chemical synthesis*
  • Anti-Ulcer Agents / pharmacology
  • Benzimidazoles / chemical synthesis*
  • Benzimidazoles / pharmacology
  • Benzoxazoles / chemical synthesis*
  • Benzoxazoles / pharmacology
  • Guinea Pigs
  • Histamine H2 Antagonists / chemical synthesis
  • Histamine H2 Antagonists / pharmacology
  • In Vitro Techniques
  • Rats
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology

Substances

  • Anti-Ulcer Agents
  • Benzimidazoles
  • Benzoxazoles
  • Histamine H2 Antagonists
  • Thiazoles