Azines and diazines as potential histamine H3-receptor antagonists

Arch Pharm (Weinheim). 1995 May;328(5):445-50. doi: 10.1002/ardp.19953280509.

Abstract

In search of structure-activity relationships among histamine H3-receptor antagonists the imidazole ring of known H3-receptor antagonists was replaced by different heteroaromatic ring systems. Thus, azines and diazines with ether (6-13) and carbamate (15-24) moieties as functional groups were synthesized. The obtained compounds did not show significant H3-receptor antagonist activity in vitro (rat brain cortex) or in vivo (mice brain). The new compounds were also screened for H1-receptor antagonist activity on the isolated guinea-pig ileum and for H2-receptor antagonist activity on the isolated spontaneously beating guinea-pig right atrium. The substances showed only weak antagonistic activity at both histamine receptors, H1 and H2.

MeSH terms

  • Animals
  • Brain Chemistry / drug effects
  • Guinea Pigs
  • Histamine Antagonists*
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • In Vitro Techniques
  • Mice
  • Muscle, Smooth / drug effects
  • Myocardial Contraction / drug effects
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • Histamine Antagonists
  • Imidazoles
  • Pyridines