85633-41-6Relevant academic research and scientific papers
α-Glucosidase inhibitory antihyperglycemic activity of substituted chromenone derivatives
Raju, B. China,Tiwari, Ashok K.,Kumar, J. Ashok,Ali, A. Zehra,Agawane, Sachin B.,Saidachary,Madhusudana
experimental part, p. 358 - 365 (2010/04/02)
Series of 3,4- and 3,6-disubstituted chromenones including new chromenone derivatives were synthesized applying various synthetic strategies including Pechmann condensation, Knoevenagel condensation, Reimer-Tiemann reaction and Suzuki coupling in very good yields. Synthesized compounds (4a-z) were screened for in vitro α-glucosidase inhibitory and 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activities. Majority of compounds displayed varying degrees of α-glucosidase inhibitory and DPPH scavenging activity. Compound 4x emerged as the most potent α-glucosidase inhibitor in present series of compounds owing to the presence of 3-acetyl-6-(6-methoxy-3-pyridyl) group on chromenone; however, it could not display DPPH scavenging activity and was found to be mixed non-competitive type inhibitor of rat intestinal α-glucosidase. When tested in vivo for antihyperglycemic activity in starch loaded Wistar rats, it displayed significant antihyperglycemic property. This is the first report assigning rat intestinal α-glucosidase inhibitory property for this class of new chromenones and presents new family of compounds possessing α-glucosidase inhibitory activities and antihyperglycemic property. Compound 4x may serve as an interesting new compound for the development of therapeutics targeted against diet-induced hyperglycemia in diabetes.
IRE-1A INHIBITORS
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Page/Page column 100; 109, (2009/01/24)
Compounds which directly inhibit IRE-lα activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
Johnson,Nidy,Aiken,Crittenden,Gorman
, p. 1461 - 1468 (2007/10/02)
The synthesis and screening of a series of 5-(3-pyridylmethyl)benzofuran-2-carboxylic acids as selective thromboxane A2 (TxA2) synthase inhibitors is outlined. The ability of these compounds to inhibit TxA2 biosynthesis was assayed using microsomal enzyme
Pyridyl-substituted-benzofurans
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, (2008/06/13)
The present invention provides novel pyridinyl-benzofurans and derivatives thereof which are useful as thromboxane A2 (TXA2) synthetase inhibitors and as such represent potent pharmacological agents.
