Quantitative structure-activity relationship study on N-(pyridin-4-yl)-(indol-3-yl) alkylamides as antiallergic agents

Indian J Biochem Biophys. 2002 Oct;39(5):351-5.

Abstract

The antihistamine activity of N-(pyridin-4-yl)-(indol-3-yl) alkylamides has been analyzed using Fujita-Ban and Hansch approaches. The analyses have helped to ascertain the role of different substituents in explaining the antiallergic actions of these analogues. From both approaches it is revealed that the small size substituents at R and R2 and non-hydrogen bond acceptor substituent at R improve histamine antagonist activity of a compound. Likewise, a small incision such as -CH2CONH-serving as the spacer between pyridinyl and indolyl rings and a bigger substituent like 4-FBn at R1 are also desirable for inhibitory activity.

MeSH terms

  • Amides / chemistry*
  • Anti-Allergic Agents / pharmacology*
  • Chemistry, Pharmaceutical / methods
  • Drug Industry / methods
  • Histamine / chemistry
  • Histamine Antagonists / pharmacology*
  • Humans
  • Hydrogen Bonding
  • Hypersensitivity / drug therapy
  • Inhibitory Concentration 50
  • Models, Chemical
  • Models, Statistical
  • Quantitative Structure-Activity Relationship
  • Structure-Activity Relationship

Substances

  • Amides
  • Anti-Allergic Agents
  • Histamine Antagonists
  • Histamine