Synthesis and biological evaluation of some new pyrazoline substituted benzenesulfonylurea/thiourea derivatives as anti-hyperglycaemic agents and aldose reductase inhibitors
| Autor: | Syed Ovais, Kalim Javed, H. Pushpalatha, Mymoona Akthar, Rafia Bashir, Pooja Rathore, Omprakash Tanwar, G. Bhanuprakash Reddy, Alhamza Dheyaa, Shafiya Yaseen, Mohammed Samim, Raed Yaseen |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Blood Glucose
Protein Conformation Stereochemistry Pyrazoline Chemistry Techniques Synthetic Inhibitory Concentration 50 chemistry.chemical_compound Aldehyde Reductase Drug Discovery Animals Hypoglycemic Agents Enzyme Inhibitors Pharmacology Aldose reductase Chemistry Organic Chemistry Thiourea General Medicine Carbon-13 NMR Rats Anti hyperglycaemic Molecular Docking Simulation Docking (molecular) Proton NMR Pyrazoles Sorbinil |
| Zdroj: | European Journal of Medicinal Chemistry. 80:209-217 |
| ISSN: | 0223-5234 |
| Popis: | 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). |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect