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

Abstract

The antihistamine activit y of N-(pyridin -4-yl)-(indol-3 -y l)

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 &nbsp;analogues. From both approaches it is revealed that the small size substituents at R and <span style="font-size:14.0pt; font-family:HiddenHorzOCR;mso-bidi-font-family:HiddenHorzOCR">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.

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