title: Design, synthesis and glucose uptake activity of some novel glitazones.
abstract: Herein, we report a library consisting of some novel glitazones containing thiazolidinedione and its bioisosteres, rhodanine and oxadiazolidine ring structures as their basic scaffold for their antidiabetic activity. Twelve novel glitazones with diverse chemical structures were designed and synthesized by adopting appropriate synthetic schemes and analyzed. Later, subjected to in vitro glucose uptake assay in the absence and presence of insulin to confirm their antidiabetic activity using rat hemi-diaphragm. The titled compounds exhibited glucose uptake activity ranging weak to significant activity. Compounds 4, 5, 9, 11, 15, 16, 19 and 20 showed considerable glucose uptake activity apart from rosiglitazone, a standard drug. Compound 16 happens to be the candidate compound from this study to investigate further. The illustration about their design, synthesis, analysis and glucose uptake activity is reported here along with the in vitro and in silico study based structure-activity relationships.
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.forename: Koyel
authors.initials: K
authors.lastname: Kar
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.forename: Uma
authors.initials: U
authors.lastname: Krithika
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.lastname: Mithuna
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.forename: Prabhuddha
authors.initials: P
authors.lastname: Basu
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.forename: S
authors.initials: S
authors.lastname: Santhosh Kumar
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1).
authors.forename: Anu
authors.initials: A
authors.lastname: Reji
authors.affiliation: Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Mysore, India; Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Ootacamund 643 001, India(1). Electronic address: brprashanthkumar@jssuni.edu.in.
authors.forename: B R
authors.initials: BR
authors.lastname: Prashantha Kumar
mesh_terms: D000818:Animals; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy* / Q000378:metabolism; D015195:Drug Design; D005260:Female; D005947:Glucose / Q000037:antagonists & inhibitors* / Q000378:metabolism; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007004:Hypoglycemic Agents; D045162:Thiazolidinediones; D005947:Glucose
keywords: Glitazones; Glucose uptake activity; Rat hemi-diaphragm; Thiazolidinediones