Novel thiophene-, pyrrole-, furan-, and benzenecarboxamidotetrazoles as potential antiallergy agents

J Med Chem. 1991 Jul;34(7):2186-94. doi: 10.1021/jm00111a039.

Abstract

The synthesis and antiallergic activity of a series of novel thiophene-, pyrrole-, furan-, and benzenecarboxamidotetrazoles are described. A number of compounds inhibit the release of histamine from anti-IgE-stimulated human basophils. Optimal inhibition is exhibited in compounds with a 3-alkoxy, a 4-halo, and a 5-methyl, 5-methoxy, or 5-bromo on a thiophene-2-carboxamidotetrazole.

MeSH terms

  • Basophils / drug effects
  • Basophils / metabolism
  • Benzene Derivatives / chemical synthesis*
  • Benzene Derivatives / pharmacology
  • Chemical Phenomena
  • Chemistry
  • Histamine H1 Antagonists / chemical synthesis*
  • Histamine H1 Antagonists / pharmacology
  • Histamine Release / drug effects
  • Humans
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Structure-Activity Relationship
  • Tetrazoles / chemical synthesis*
  • Tetrazoles / pharmacology
  • Thiophenes / chemical synthesis*
  • Thiophenes / pharmacology

Substances

  • Benzene Derivatives
  • Histamine H1 Antagonists
  • Pyrroles
  • Tetrazoles
  • Thiophenes