title: Thiazolidin-4-one and thiazinan-4-one derivatives analogous to rosiglitazone as potential antihyperglycemic and antidyslipidemic agents.
abstract: A number of thiazolidin-4-one and thiazinan-4-one derivatives were prepared by three component condensation in one pot reaction method. These compounds were evaluated for anti-hyperglycemic activity by in vitro and in vivo assay systems. The compounds with thiazolidin-4-one and thiazinan-4-one moieties exhibited significant anti-hyperglycemic activity. A few compounds (3a, 3b, 4a and 4b) have exhibited both anti-hyperglycemic and anti-dyslipidemic activities. Among them the thiazinan-4-one derivative 4a showed maximal (45%) improvement in oral glucose tolerance test in db/db mice at 30 mg/kg oral dose.
authors.affiliation: Medicinal and Process Chemistry Division, CSIR - Central Drug Research Institute, Lucknow 226001, India.
authors.forename: Saman
authors.initials: S
authors.lastname: Raza
authors.forename: Swayam P
authors.initials: SP
authors.lastname: Srivastava
authors.forename: Daya S
authors.initials: DS
authors.lastname: Srivastava
authors.forename: Arvind K
authors.initials: AK
authors.lastname: Srivastava
authors.forename: W
authors.initials: W
authors.lastname: Haq
authors.forename: S B
authors.initials: SB
authors.lastname: Katti
mesh_terms: D041721:3T3-L1 Cells; D000818:Animals; D001786:Blood Glucose / Q000378:metabolism; D002454:Cell Differentiation / Q000187:drug effects; D002460:Cell Line; D003924:Diabetes Mellitus, Type 2 / Q000097:blood / Q000517:prevention & control; D004305:Dose-Response Relationship, Drug; D050171:Dyslipidemias / Q000517:prevention & control; D005947:Glucose / Q000378:metabolism / Q000493:pharmacokinetics; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008956:Models, Chemical; D015394:Molecular Structure; D018482:Muscle, Skeletal / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D000077154:Rosiglitazone; D013329:Structure-Activity Relationship; D013843:Thiazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045162:Thiazolidinediones / Q000737:chemistry / Q000494:pharmacology; D053778:Thiazolidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014280:Triglycerides / Q000097:blood
chemical_list: D001786:Blood Glucose; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D013843:Thiazines; D045162:Thiazolidinediones; D053778:Thiazolidines; D014280:Triglycerides; D000077154:Rosiglitazone; D005947:Glucose