Journal
FUTURE MEDICINAL CHEMISTRY
Volume 15, Issue 1, Pages 9-24Publisher
Newlands Press Ltd
DOI: 10.4155/fmc-2022-0141
Keywords
antidiabetic; docking; DPP-IV; in silico; oral glucose tolerance test; pyrazoline
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In this study, a series of analogues were synthesized and evaluated, and KB-23, KB-22, and KB-06 showed promising antihyperglycemic potential in both in vitro and in vivo studies, making them potential starting points for the development of antidiabetic agents.
Background: Mining of novel scaffolds as potential DPP-IV inhibitors for future development of potential candidates as antidiabetic agents to address global issues. Methodology: The identified hit KB-10 from a previously reported study was taken as a lead for designing a library of analogues and screened initially based on in silico parameters and docking score. A series of selected (2[4-(1-acetyl-5-phenyl-4,5-dihydro-1H-pyrazol-3-yl)phenoxy]-1-phenylethanone derivatives were synthesized and evaluated through in vitro studies. Compounds KB-23, KB-22 and KB-06 were found to be as potent, with IC50 values of 0.10 mu M, 0.12 mu M and 0.35 mu M, respectively. They also showed promising antihyperglycemic potential in in vivo studies (oral glucose tolerance tests) in Wistar rats. Conclusion: This work establishes pyrazoline analogues KB-23, KB-22 and KB-06 as promising starting points for the development of potential antidiabetic agents.
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