Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents

Sharma Shweta; Ansari Mohd. Hafizur Rehman; Sharma KalicharanSingh Rajesh K.Ali ShakirAlam Mohd. MumtazZaman Mohd. ShaqiquzammanAlam PrawezAkhter Mymoona

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Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents

机译：Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents

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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 (24-(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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《Future medicinal chemistry》 |2023年第1期|9-24|共16页
作者
Sharma Shweta; Ansari Mohd. Hafizur Rehman; Sharma KalicharanSingh Rajesh K.Ali ShakirAlam Mohd. MumtazZaman Mohd. ShaqiquzammanAlam PrawezAkhter Mymoona;
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作者单位

Jamia Hamdard University,Jamia Hamdard;

Dept Pharmaceut Chem,Shivalik Coll Pharm;

Sch Chem & Biol Sci,Jamia HamdardDept Pharmacognosy,Prince Sattam Bin Abdulaziz Univ;

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正文语种英语
中图分类药学;
关键词
antidiabetic; docking; DPP-IV; in silico; oral glucose tolerance test; pyrazoline; DIPEPTIDYL-PEPTIDASE-IV; SCREENING LIBRARIES; INHIBITORS; DISCOVERY; POTENT; ANALOGS; DESIGN;

Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents

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