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Design and Synthesis of Pyrazole-3-one Derivatives as Hypoglycaemic Agents
Author(s) -
Prasanna A. Datar,
Sonali R. Jadhav
Publication year - 2015
Publication title -
international journal of medicinal chemistry
Language(s) - English
Resource type - Journals
eISSN - 2090-2069
pISSN - 2090-2077
DOI - 10.1155/2015/670181
Subject(s) - pyrazole , docking (animal) , metformin , chemistry , in vivo , stereochemistry , combinatorial chemistry , diabetes mellitus , medicine , biology , nursing , microbiology and biotechnology , endocrinology
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.

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