title: Flavone-based novel antidiabetic and antidyslipidemic agents.
abstract: The hybrid congeners 62-90 of 6- and 7-hydroxyflavones with aminopropanol have been synthesized and evaluated for their antidiabetic activity in sucrose-challenged low-dosed streptozotocin (STZ)-induced diabetic rats and db/db mice. The optical enantiomers 70a, 70b, 90a, and 90b of two congeners 70 and 90 exhibiting consistent antidiabetic and antidyslipidemic activities were also prepared, and their antidiabetic activity results indicate its association mainly with S isomers. These compounds also lower cholesterol and TG profiles while improving high-density lipoprotein cholesterol to CHOL ratio in db/db mice. The bioavailability of compound 70 and its isomer varies between 27 and 29% whereas that of the more polar compound 90a is poor as determined in rat by oral and intraperitoneal administrations.
authors.affiliation: Division of Medicinal & Process Chemistry, Central Drug Research Institute (CSIR), Lucknow-226001, India.
authors.forename: Alok K
authors.initials: AK
authors.lastname: Verma
authors.forename: Himanshu
authors.initials: H
authors.lastname: Singh
authors.forename: Mavurapu
authors.initials: M
authors.lastname: Satyanarayana
authors.forename: Swayam P
authors.initials: SP
authors.lastname: Srivastava
authors.forename: Priti
authors.initials: P
authors.lastname: Tiwari
authors.forename: Amar B
authors.initials: AB
authors.lastname: Singh
authors.forename: Anil K
authors.initials: AK
authors.lastname: Dwivedi
authors.forename: Shio K
authors.initials: SK
authors.lastname: Singh
authors.forename: Mukesh
authors.initials: M
authors.lastname: Srivastava
authors.forename: Chandishwar
authors.initials: C
authors.lastname: Nath
authors.forename: Ram
authors.initials: R
authors.lastname: Raghubir
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: Ram
authors.initials: R
authors.lastname: Pratap
mesh_terms: D000818:Animals; D001682:Biological Availability; D002784:Cholesterol / Q000097:blood; D006224:Cricetinae; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy*; D004305:Dose-Response Relationship, Drug; D047309:Flavones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007328:Insulin / Q000097:blood; D008297:Male; D008647:Mesocricetus; D051379:Mice; D008810:Mice, Inbred C57BL; D051381:Rats; D017207:Rats, Sprague-Dawley; D017208:Rats, Wistar; D013237:Stereoisomerism; D013311:Streptozocin; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood
chemical_list: D047309:Flavones; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D007328:Insulin; D014280:Triglycerides; D013311:Streptozocin; D002784:Cholesterol