174258-63-0Relevant articles and documents
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.
New azolidinediones and thiadiazolidinediones as antihyperglycemic agents
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, (2008/06/13)
This invention relates to novel compounds which have demonstrated oral antihyperglycemic activity in diabetic ob/ob and db/db mice, animal models on non-insulin dependent diabetes mellitus (NIDDM ot Type II diabetes). These compounds have the formula: STR1 wherein: R1 is C1 -C6 alkyl, C3 -C8 cycloalkyl, thienyl, furyl, pyridyl, STR2 where R10 is hydrogen, C1 -C6 alkyl, fluorine, chlorine, bromine, iodine, C1 -C6 alkyoxy, trifluoroalkyl or trifluoroalkoxy; R2 is hydrogen or C1 -C6 alkyl; X is O or S; n is 0, 1, or 2; A is STR3 where R3 is hydrogen, C1 -C6 alkyl, halogen, C1 -C6 alkoxy, trifluoroalkyl or trifluoroalkoxy; B is STR4 where R4 is hydrogen, C1 -C6 alkyl, allyl, C6 -C10 aryl, C6 -C10 aryl-(CH2)1-6 --, fluorine, chlorine, bromine, iodine, trimethylsilyl or C3 -C8 cycloalkyl; R5 is hydrogen, C1 -C6 alkyl, C6 -C10 aryl, or C6 -C10 aryl-(CH2)1-6 --; m is 0, 1, or 2; R6 is hydrogen or C1 -C6 alkyl; R7 is hydrogen or C1 -C6 alkyl; R8 and R9 are selected independently from hydrogen, C1 -C6 alkyl, fluorine, chlorine, bromine, or iodine; Y is S; Z is N or CH; or a pharmaceutically acceptable salt thereof.