title: Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.
authors.forename: Alaa A-M
authors.initials: AA
authors.lastname: Abdel-Aziz
authors.forename: Adel S
authors.initials: AS
authors.lastname: El-Azab
authors.forename: Sabry M
authors.initials: SM
authors.lastname: Attia
authors.forename: Abdulrahman M
authors.initials: AM
authors.lastname: Al-Obaid
authors.forename: Mohamed A
authors.initials: MA
authors.lastname: Al-Omar
authors.forename: Hussein I
authors.initials: HI
authors.lastname: El-Subbagh
mesh_terms: D000818:Animals; D001786:Blood Glucose / Q000032:analysis; D004353:Drug Evaluation, Preclinical; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007928:Lethal Dose 50; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents