SYNTHESIS OF SOME NEW DERIVATIVES OF ISOINDOLINE-1,3-DIONE NUCLEUS FOR ANTIHYPERGLYCEMIC EVALUATION | ||||
| Al-Azhar Journal of Pharmaceutical Sciences | ||||
| Article 9, Volume 48, Issue 2 - Serial Number 48, September 2013, Page 120-129 PDF (349.85 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/ajps.2013.7100 | ||||
 View on SCiNiTO | ||||
| Author | ||||
| Ibrahim Eissa | ||||
| Pharmaceutical Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt | ||||
| Abstract | ||||
| In order to produce potent new leads for antidiabetic drugs, a new series of isoindoline-1,3-dione analogues bearing aryl sulfonylurea moieties were synthesized and screened for their antihyperglycemic activity. Some of newly synthesized compounds were identified as active antihyperglycemic agents. Compounds N-(cyclohexylcarbamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl) ethyl]benzenesulfon-amide(VIIo),N-(cyclopentylcabamoyl)-4-[2-(1,3-dioxoiso- indolin-2-yl)ethyl] benzene sulfonamide (VIIp), N-(butylcabamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl)ethyl]benzenesulfonamide(VIIq),N-(cyclohexylcarbamoyl) -4- [ ( 1, 3- dioxo - isoindolin- 2 – yl ) methyl ] benzenesulfonamide (VIIh) and N-(propylcabamoyl)-4-[2-(1,3-dioxoisoindolin-2-yl)ethyl]benzenesulfonamide (VIIr) proved to be the most active members of this study, as compered to to the reference gliclazide. They showed serum glucose reduction values of 52%, 48% 45%, 44% and 44%, respectively. The detailed synthesis and biological screening data are reported. | ||||
| Keywords | ||||
| Isoindoline-1,3-diones; Sulfonylurea; Antihyperglycemic activity | ||||
|
Statistics Article View: 163 PDF Download: 191 |
||||
