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- Title
Synthesis, Enzyme Inhibition, and Molecular Docking Studies of Hydrazones from Dichlorophenylacetic Acids.
- Authors
Abid, Obaid‐ur‐Rahman; Ayaz, Muhammad; Rehman, Wajid; Mehdi, Kamran; Ali, Arif; Wadood, Abdul; Rahim, Fazal; Sultan, Aneesa; Ghufran, Mehreen; Mir, Sadullah; Qureshi, Muhammad Tauseef
- Abstract
A series of hydrazones 5a-i were synthesized by the condensation of hydrazides derived from dichlorophenylacetic acids with different aromatic aldehydes and ketones. Their structures were confirmed by spectroscopic data and elemental analysis. Hydrazones 5a-i were evaluated for α-glucosidase and urease inhibition activities. Five compounds exhibited potent α-glucosidase inhibitory potential with IC50 values 8.5 ± 0.3, 22.2 ± 0.78, 32.9 ± 1.5, 34 ± 2.4, and 170.6 ± 7.5 μM, respectively, which are many times better than that of the standard inhibitor acarbose ( IC50 = 840 ± 1.73 μM). Furthermore, molecular docking study was performed to explore the binding mode in the active sites of α-glucosidase and urease enzymes.
- Subjects
HYDRAZONES; MOLECULAR docking; ENZYMES; CHEMICAL synthesis; CONDENSATION; GLUCOSIDASES
- Publication
Journal of the Chinese Chemical Society, 2016, Vol 63, Issue 12, p1015
- ISSN
0009-4536
- Publication type
Article
- DOI
10.1002/jccs.201600163