Abstract
BRONCHOSPASMOLYTIC ACTIVITY OF 8-PHENYL SUBSTITUTED (SULPHONAMIDE) XANTHINE DERIVATIVES

Divya Gumber and Rakesh Yadav*

ABSTRACT

Background: A series of suplhonamide substituted xanthine derivatives were synthesized. The introduction of the heterocyclic spacers in the xanthine skeleton at C-8 improves therapeutic profile. The incorporation of polar substituents such as sulfonates was done in order to improve the limited water solubility of xanthines. Further incorporation of spacers like heteroatoms (nitrogen and sulphur) provided additional sites of interaction thus giving the desired selectivity with increased potency. Findings: The structures of the newly synthesized compounds were characterized by TLC, FT-IR, 1H & 13C-NMR and elemental analyses. The synthesized derivatives were also evaluated in vivo for bronchospasmolytic activity. Among the derivatives 8a-f, the animals treated with compound 8f showed more protective action in the histamine induced bronchospasm. Increased bulkiness on the p-position of the aromatic ring increases the bronchospasmolytic activity. Conclusion: The sulfonamide derivatives of 8-phenylsubstituted xanthines were synthesized and evaluated for their bronchospasmolytic activity.

Keywords: Xanthines, Sulphonamide, Bronchospasmolytic, Anti-asthmatics.


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