2024
DOI: 10.3389/fchem.2024.1387923
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Design and synthesis of new dihydropyrimidine/sulphonamide hybrids as promising anti-inflammatory agents via dual mPGES-1/5-LOX inhibition

Lamya H. Al-Wahaibi,
Ali M. Elshamsy,
Taha F. S. Ali
et al.

Abstract: A novel series of dihydropyrimidine/sulphonamide hybrids 3a–j with anti-inflammatory properties have been developed and tested as dual mPGES-1/5-LOX inhibitors. In vitro assay, results showed that compounds 3c, 3e, 3h, and 3j were the most effective dual inhibitors of mPGES-1 and 5-LOX activities. Compound 3j was the most potent dual inhibitor with IC50 values of 0.92 µM and 1.98 µM, respectively. In vivo, anti-inflammatory studies demonstrated that compounds 3c, 3e, 3h, and 3e had considerable anti-inflammato… Show more

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