Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 11, 2010, Pages 3420-3425

  Kim, Min Ju ^a   Lee, Junwon ^a   Kang, Suk Youn ^a   Lee, Sung Han ^a   Son, Eun Jung ^a   Jung, Myung Eun ^a   Lee, Suk Ho ^a   Song, Kwang Seop ^a   Lee, MinWoo ^a   Han, Ho Kyun ^a   Kim, Jeongmin ^a   Lee, Jinhwa ^a  

^a Green Cross Company   (South Korea)

Author keywords

Dapagliflozin; Diabetes; Glucoside; Pyridazine; SGLT

Indexed keywords

ANTIDIABETIC AGENT; CANAGLIFLOZIN; DAPAGLIFLOZIN; GLUCOSE; PYRIDAZINE; SODIUM GLUCOSE COTRANSPORTER 2 INHIBITOR; THIADIAZOLE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INHIBITION; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; GLUCOSE URINE LEVEL; GLUCOSURIA; IN VITRO STUDY; IN VIVO STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; RAT;

ANIMALS; GLUCOSIDES; HYPOGLYCEMIC AGENTS; RATS; RATS, SPRAGUE-DAWLEY; SODIUM-GLUCOSE TRANSPORTER 2;

RATTUS;

EID: 77953287835     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.04.006     Document Type: Article

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28. 20-22 Male SD rats weighing 250-300 g (7-8 weeks old) were purchased from Orient-Bio Laboratory Animal Research Center Co. (Gyeonggi-do, Korea). They were housed in a temperature (25 ± 2 °C), and moisture (55 ± 10%) controlled room, exposed to a controlled 12 h cycle of light and darkness, and allowed free access to food and water. All animals were acclimated for one week prior to the experiment. For glucosuria assessment, overnight-fasted SD rats were placed into metabolism cages for baseline urine collection over 24 h. Rats were weighed, randomized into three groups in plane (n = 3), dosed orally with single doses of vehicle or drug (1 @1 mg/kg, 32l @10 mg/kg), and subsequently dosed orally with 50% aqueous glucose solution (2 g/kg). Immediately after dosing, rats were returned to the metabolism cages for 24 h urine collection and re-fed at 1 h after the glucose challenge.
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