Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents

被引:53
|
作者
Abdel-Aziz, Alaa A. -M. [1 ,2 ]
El-Azab, Adel S. [1 ,3 ]
Attia, Sabry M. [4 ,5 ]
Al-Obaid, Abdulrahman M. [1 ]
Al-Omar, Mohamed A. [1 ]
El-Subbagh, Hussein I. [1 ,2 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut Chem, Riyadh 11451, Saudi Arabia
[2] Univ Mansoura, Fac Pharm, Dept Med Chem, Mansoura 35516, Egypt
[3] Al Azhar Univ, Fac Pharm, Dept Organ Chem, Cairo 11884, Egypt
[4] King Saud Univ, Coll Pharm, Dept Pharmacol, Riyadh 11451, Saudi Arabia
[5] Al Azhar Univ, Fac Pharm, Dept Pharmacol, Cairo 11884, Egypt
关键词
Synthesis; Isoindolinediones; Tetrahydro-methyl-isoindolediones; Hypoglycaemic; Anti-hyperlipidemic agents; HIGH-YIELDING SYNTHESIS; CORONARY-HEART-DISEASE; HYPOLIPIDEMIC ACTIVITY; INSULIN-RESISTANCE; N-ALKYL; ACID; TRIGLYCERIDES; DYSLIPIDEMIA; PHTHALIMIDES; CHOLESTEROL;
D O I
10.1016/j.ejmech.2011.07.002
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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 Se remarkably reduced serum glucose level by 55%; while 5c, Se, 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. (C) 2011 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码:4324 / 4329
页数:6
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