Affordable Access

Publisher Website

SAR studies on H2antagonists containing alkylamino substituted 1,2,5-thiadiazole 1-oxide moieties

Authors
Journal
Il Farmaco
0014-827X
Publisher
Elsevier
Publication Date
Volume
53
Identifiers
DOI: 10.1016/s0014-827x(98)00059-7
Keywords
  • H2Antagonists
  • Ranitidine Analogues
  • Sar In H2Antagonists

Abstract

Abstract A number of ranitidine analogues in which the diamino-1,2,5-thiadiazole 1-oxide substructure bearing alkyl chains of different length is present as the urea equivalent group, were synthesised and studied for their lipophilic and H 2 antagonist properties. Derivatives which displayed a log P≤3 behaved as competitive antagonists of histamine at H 2 receptors present on guinea pig right atrium. The remaining more lipophilic members of the series showed an insurmountable antagonism not completely reversible after prolonged washing. A binding study suggested that an increase in the length of alkyl chain gave rise to hydrophobic interactions with the receptor which were responsible for the apparent irreversible H 2 antagonism shown by the higher homologues of the series.

There are no comments yet on this publication. Be the first to share your thoughts.