159017-97-7Relevant 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.
Thiazolidinedione derivatives, their production and use
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, (2008/06/13)
A 2,4-thiazolidinedione derivative of the formula (I): STR1 wherein R is an optionally substituted hydrocarbon group or heterocyclic group which may be attached through a hydrocarbon chain; n is 0 or 1; X is CH or N; Y is a bivalent hydrocarbon group; Rs
Oxazolidinedione derivatives and their use
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, (2008/06/13)
Novel 2,4-oxazolidinedione compounds of the formula: STR1 wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is --CO--, --CH(OH)-- or --NR3 -- (wherein R3 is an alkyl group which may be substituted); m is 0 or 1; n is 0, 1 or 2; X is CH or N; A is bivalent straight or branched hydrocarbon chain residue having 1 to 7 carbon atoms; R1 and R2 each are hydrogen or an alkyl group, or R1 and R2 are combined with each other to form a 5- to 6-membered heterocyclic group optionally containing nitrogen; L and M each are hydrogen, or L and M are combined with each other to form a bond, or pharmaceutically acceptable salts thereof, having excellent hypoglycemic and hypolipidemic activities and are useful as anti-diabetics or hypolipidemic agents.
Azole phenoxy hydroxyureas as selective and orally active inhibitors of 5- lipoxygenase
Malamas,Carlson,Grimes,Howell,Glaser,Gunawan,Nelson,Kanzelberger,Shah,Hartman
, p. 237 - 245 (2007/10/03)
Azole phenoxy hydroxyureas are a new class of 5-lipoxygenase (5-LO) inhibitors. Structure-activity relationship studies have demonstrated that electronegative substituents on the 2-phenyl portion of the oxazole tail increased the ex vivo potency of these
