412300-65-3Relevant academic research and scientific papers
Novel thiazolidinedione derivatives with anti-obesity effects: Dual action as PTP1B inhibitors and PPAR-γ activators
Bhattarai, Bharat Raj,Kafle, Bhooshan,Hwang, Ji-Sun,Ham, Seung Wook,Lee, Keun-Hyeung,Park, Hwangseo,Han, Inn-Oc,Cho, Hyeongjin
supporting information; experimental part, p. 6758 - 6763 (2010/12/20)
Benzylidene-2,4-thiazolidinedione derivatives with substitutions at both the ortho and para-positions of the phenyl group were synthesized as PTP1B inhibitors with IC50 values in a low micromolar range. Compound 18l, the lowest, bore an IC50 of 1.3 μM. In a peroxisome proliferator-activated receptor-γ (PPAR-γ) promoter reporter gene assay, 18l was found to activate the transcription of the reporter gene with potencies comparable to those of troglitazone, rosiglitazone, and pioglitazone. In vivo efficacy of 18l as an anti-obesity and hypoglycemic agent was evaluated in a mouse model system. Compound 18l significantly suppressed weight gain and significantly improved blood parameters such as TG, total cholesterol and NEFA without overt toxic effects.
VITAMIN D RECEPTOR MODULATORS
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Page/Page column 131-132, (2008/06/13)
The present invention relates to novel, non-secosteroidal, phenyl-benzofuran compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
