کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1394101 | 1501136 | 2014 | 9 صفحه PDF | دانلود رایگان |
• Seventeen new pyrazoline substituted benzenesulfonylurea/thiourea derivatives (2a–q) were synthesized.
• Thirteen compounds showed moderate to good anti-hyperglycaemic activity.
• Compounds 2g and 2m showed anti-hyperglycaemic activity comparable to the standard drug gliclazide.
• Six compounds (2h, 2k, 2l, 2n, 2o and 2q) were found more effective ARIs than the known ARI sorbinil.
• Five compounds (2h, 2k, 2l, 2n and 2o) showed dual action (anti-hyperglycaemic and aldose reductase inhibition).
Seventeen new pyrazoline substituted benzenesulfonylurea/thiourea derivatives (2a–q) were synthesized and characterized by elemental analysis and various spectroscopic techniques viz; IR, 1H NMR, 13C NMR, and MS data. Thirteen compounds showed moderate to good anti-hyperglycaemic activity in glucose fed hyperglycaemic normal rats at the dose of 0.05 mM/kg b.w. On the basis of docking results nine compounds (2a, 2c, 2e, 2h, 2k, 2l, 2n, 2o and 2q) were evaluated for their ability to inhibit rat lens aldose reductase. Out of these six compounds (2h, 2k, 2l, 2n, 2o and 2q) were found more effective than the known ARI sorbinil. Five compounds (2h, 2k, 2l, 2n and 2o) showed significant dual action (anti-hyperglycaemic and aldose reductase inhibition).
Five compounds (2h, 2k, 2l, 2n and 2o) showed significant dual action (anti-hyperglycaemic and ARI). Two compounds 2g and 2m showed anti-hyperglycaemic activity comparable to standard drug gliclazide.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 80, 10 June 2014, Pages 209–217