4.2 Article

Synthesis and SAR studies of potent H+/K+-ATPase and anti-inflammatory activities of symmetrical and unsymmetrical urea analogues

Journal

MEDICINAL CHEMISTRY RESEARCH
Volume 26, Issue 8, Pages 1675-1681

Publisher

SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-017-1878-x

Keywords

Ureas's; SAR; H+/K+-ATPase; anti-inflammatory

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A sequence of symmetrical and unsymmetrical urea derivatives 1-24 were synthesized and characterized by standard spectroscopic techniques. The synthesized analogues were tested for their in vitro H+/K+-ATPase and anti-inflammatory activities. The majority of the compounds showed outstanding activity, compared to that of omeprazole and indomethacin, usual standard drugs of antiulcer and anti-inflammatory, respectively. In particular, hydroxy, methyl, and methoxy derivatives 13-24 were the most active compounds possessing a significant amplify for diverse substituents on the benzene ring thus, contributing positively to gastric ulcer inhibition. Compounds 1-3 and 22-24 showed excellent anti-inflammatory activity due to the presence of electron-withdrawing groups (Cl and F) on the molecule.

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