Quantitative structure-activity relationship study on N-(pyridin-4-yl)-(indol-3-yl) alkylamides as antiallergic agents.
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.
Department of Chemistry, S.K. Government College, Sikar 332 001, India.
P
P
Singh
B K
BK
Sharma
R
R
Kumar
D000577:Amides / Q000737:chemistry*; D018926:Anti-Allergic Agents / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004345:Drug Industry / Q000379:methods; D006632:Histamine / Q000737:chemistry; D006633:Histamine Antagonists / Q000494:pharmacology*; D006801:Humans; D006860:Hydrogen Bonding; D006967:Hypersensitivity / Q000188:drug therapy; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015233:Models, Statistical; D021281:Quantitative Structure-Activity Relationship; D013329:Structure-Activity Relationship
D000577:Amides; D018926:Anti-Allergic Agents; D006633:Histamine Antagonists; D006632:Histamine