Journal
MEDICINAL CHEMISTRY RESEARCH
Volume 24, Issue 3, Pages 1310-1324Publisher
SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-014-1213-8
Keywords
2-Methoxybenzoylhydrazone; alpha-Glucosidase; Urease; Crystal structure
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Funding
- Research Management Institute of UiTM under CIFI [600-RMI/DANA5/3/CIFI (141/2013)]
- Organization for The Prohibition of Chemical Weapons (OPCW), The Netherlands [L/ICA/ICB/173681/12]
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Compounds 1-30 showed varying degree of alpha-glucosidase inhibition with IC50 values ranging between 187 and 420 mu M. Compounds 1, 2, 3, 6, 8, 12, and 4 (IC50 = 187.7 +/- A 3.05, 203.4 +/- A 4.0, 240.7 +/- A 1.9, 252.9 +/- A 3.9, 285.2 +/- A 6.3, 399.07 +/- A 1.2, and 420.36 +/- A 5.6 mu M, respectively) were found to be more active than standard acarbose (IC50 = 906 +/- A 6.3 mu M). The synthetic compounds were also tested for urease inhibition. Compounds 5 (IC50 = 19.6 +/- A 1.0 mu M) and 1 (IC50 = 21.6 +/- A 0.6 mu M) showed better activity than standard drug thiourea (IC50 = 21.8 +/- A 1.6 mu M). The crystal structures of compounds 15 and 16 are also reported. Compounds 1-30 synthesized and evaulated for Alpha-glucosidase as well as Ureas inhibition. The crystal structures of compounds 15 and 16 are also reported.
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