Journal
BIOORGANIC CHEMISTRY
Volume 86, Issue -, Pages 197-209Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2019.01.040
Keywords
1,3-Thiazole; 1,2,4-Triazole; Acetamides; Elastase; Kinetics; Molecular docking
Funding
- Basic Science Research Program through the National Research Foundation of Korea (NRF) - Ministry of Education, South Korea [2017R1D1A1B03034948]
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Keeping in mind the pharmacological importance of 2-aminothiazole and 1,2,4-triazole heterocyclic moieties, a series of novel ethylated bi-heterocyclic acetamide hybrids, 9a-p, was synthesized in a multi-step protocol. The structures of newly synthesized compounds were characterized by H-1 NMR, C-13 NMR, IR and EI-MS spectral studies. The inhibitory effects of these bi-heterocyclic acetamides (9a-n) were evaluated against elastase and all these molecules were identified as potent inhibitors relative to the standard used. The Kinetics mechanism was analyzed by Lineweaver-Burk plots which revealed that, 9h, inhibited elastase competitively by forming an enzyme-inhibitor complex. The inhibition constants K-i calculated from Dixon plots for this compound was 0.9 mu M. The computational study was articulate with the experimental results and these ligands unveiled good binding energy values (kcal/mol). So, these molecules can be considered as promising medicinal scaffolds for the treatment of skin melanoma, wrinkle formation, uneven pigmentation, and solar elastosis.
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