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

International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-02-04 DOI:10.1155/2015/670181
Prasanna A Datar, Sonali R Jadhav
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引用次数: 25

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.

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降血糖药吡唑-3-酮衍生物的设计与合成。
吡唑-3- 1化合物是在先前报道的抗糖尿病吡唑化合物对接研究的基础上设计的。对接研究中发现的氨基酸残基可作为吡唑-3- 1结构芳香取代修饰的指导。根据对接分数,设计的化合物被选择性地优先合成。以四氧嘧啶诱导的糖尿病大鼠和二甲双胍为标准,对合成的化合物进行体内降糖活性研究。具有磺胺衍生物的化合物4是该系列化合物中最有效的化合物。
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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