|
|||||
|
|
Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents |
|
| Authors: | Abdel-Aziz Alaa A-M El-Azab Adel S Attia Sabry M Al-Obaid Abdulrahman M Al-Omar Mohamed A El-Subbagh Hussein I |
| Affiliation: | a Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia b Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura 35516, Egypt c Department of Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt d Department of Pharmacology, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia e Department of Pharmacology, Faculty of Pharmacy, Al-Azhar University, Cairo 11884, Egypt |
| Abstract: | Certain new halogenated cyclic-imides related to N-substituted phthalimide moiety were synthesized. Spacers of one or two carbon atom distances were inserted to connect the N-terminus of the cyclic-imide nuclei to the used heteroaryl groups to evaluate the effect of such alteration on biological activity. The synthesized compounds were subjected to hypoglycaemic and anti-hyperlipidemic evaluation. Some of the tested compounds proved to be more potent than the reference drugs glibenclamide and clofibrate. Compound 5e remarkably reduced serum glucose level by 55%; while 5c, 5e, 7d and 8e reduced total serum cholesterol by 58, 56, 54 and 53%, respectively. Those new cyclic-imides could be considered as useful template for future development to obtain more potent hypoglycaemic and anti-hyperlipidemic agents. |
| Keywords: | Synthesis Isoindolinediones Tetrahydro-methyl-isoindolediones Hypoglycaemic Anti-hyperlipidemic agents |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |