132646-34-5Relevant academic research and scientific papers
Antihyperglycemic activity of new 1,2,4-oxadiazolidine-3,5-diones
Malamas, Michael S,Sredy, Janet,McCaleb, Michael,Gunawan, Iwan,Mihan, Brenda,Sullivan, Donald
, p. 31 - 42 (2007/10/03)
A series of 1,2,4-oxadiazolidine-3,5-diones was synthesized and evaluated as oral antihyperglycemic agents in the obese insulin resistant db/db and ob/ob mouse - the two models for Type 2 diabetes mellitus. The majority of the prepared methoxy- and ethoxy-linked oxazole 1,2,4-oxadiazolidine-3,5-diones normalized plasma glucose levels at the 100 mg kg-1 oral dose in the db/db diabetic mouse model, and several amongst them reduced the glucose levels at the 20 mg kg-1 oral dose. The most potent compounds in the db/db mouse model were also active in the ob/ob mouse model normalizing the plasma glucose levels at the 20 mg kg-1 oral dose. The trifluoromethoxy analog 32 was the most active compound of the series, reducing significantly the plasma glucose levels at the 5 mg kg-1 oral dose. Oxadiazole-tailed 1,2,4-oxadiazolidine-3,5-diones were also active in both the db/db and ob/ob diabetic mouse models normalizing plasma glucose levels at the 100 mg kg-1 oral dose.
Hypoglycemic activity of a series of α-alkylthio and α-alkoxy carboxylic acids related to ciglitazone
Hulin, Bernard,Newton, Linda S.,Lewis, Diana M.,Genereux, Paul E.,Gibbs, E. Michael,Clark, David A.
, p. 3897 - 3907 (2007/10/03)
The thiazolidinedione moiety of ciglitazone and its analogues can be replaced by an α-alkoxy or α-thioether carboxylic acid group. The influence of the nature of the R group, the length of the connector to the aromatic backbone of the molecule, and the stereochemistry have been studied. The most potent compounds have glucose-lowering activity at doses as low as 0.01 mg/kg.
Oxazolidinedione hypoglycemic agents
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, (2008/06/13)
Compounds of the formulae STR1 where R is cycloalkyl or aryl; R1 is alkyl, X is O or C=O; A is O or S; and B is N or CH are useful as hypoglycemic agents.
Hypoglycemic hydroxyurea derivatives
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, (2008/06/13)
There are disclosed preparative processes and hypoglycemic compounds of the formula STR1 wherein R is hydrogen or C1 to C3 alkyl; R1 and R2 are taken together and are carbonyl; or R1 and R2 are taken separately, wherein R1 is hydrogen or R4 and R2 is--COR5 and COOR5 ; R3, R4 and R5 are each independently C1 to C9 alkyl, C3 to C7 cycloalkyl, phenyl, naphthyl, furyl, benzofuryl or thienyl or one of said groups mono- or disubstituted with C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 alkoxy-carbonyl, trifluoromethyl, fluoro or chloro; and n is 0 or 1; or pharmaceutically acceptable cationic salts thereof.
3-aryl-2-hydroxypropionic acid derivatives and analogs as antihypertensives
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, (2008/06/13)
A method of using certain 3-aryl-2-hydroxypropionic acid derivatives and analogs in the treatment of hypertension.
3-coxazolyl [phenyl, chromanyl or benzofuranyl]-2-hydroxypropionic acid derivatives and analogs as hypoglycemic agents
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, (2008/06/13)
Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl, or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.
Benzyloxazolidine-2,4-diones as potent hypoglycemic agents
Dow,Bechle,Chou,Clark,Hulin,Stevenson
, p. 1538 - 1544 (2007/10/02)
A series of benzyloxazolidine-2,4-diones, containing oxazole-based side chains, were found to lower blood glucose levels in the genetically obese ob/ob mouse. Incorporation of a benzofuran structural element in these compounds provides greatly enhanced in vivo potency. The syntheses and structure-activity relationships for this series are detailed.
Oxazolidinedione hypoglycemic agents
-
, (2008/06/13)
Compounds of the formulae where R is cycloalkyl or aryl; R1 is alkyl, X is O or C=O; A is O or S; and B is N or CH are useful as hypoglycemic agents.
