Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents

International Journal of Medicinal Chemistry
Prasanna A Datar, Sonali R Jadhav

Abstract

Pyrazole-3-one compounds were designed on the basis of docking studies of previously reported antidiabetic pyrazole compounds. The amino acid residues found during docking studies were used as guidelines for the modification of aromatic substitutions on pyrazole-3-one structure. Depending on the docking score, the designed compounds were selectively prioritized for synthesis. The synthesized compounds were subjected to in vivo hypoglycemic activity using alloxan induced diabetic rats and metformin as a standard. Compound 4 having sulphonamide derivative was found to be the most potent compound among the series.

References

Jul 20, 2002·Bioorganic & Medicinal Chemistry Letters·Bertrand CottineauJacques Chenault
Jul 23, 2003·Current Medicinal Chemistry·V Melih Altan
Mar 10, 2009·European Journal of Medicinal Chemistry·Mohamed Abdel-AzizAlaa A Hassan
May 8, 2009·European Journal of Medicinal Chemistry·Osama I el-SabbaghAdel A Rashad
Oct 4, 2011·The Open Medicinal Chemistry Journal·Ernest Adeghate
Feb 7, 2013·European Journal of Medicinal Chemistry·A M VijeshHoong Kun Fun

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Citations

Feb 13, 2018·Indian Journal of Microbiology·Jagdish R BadgujarJyotsna S Meshram

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Methods Mentioned

BETA
X-ray
NMR

Software Mentioned

GlideScore
Graph pad
Schrodinger
Glide

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