158093-66-4Relevant academic research and scientific papers
SYNTHESIS OF 2-SUBSTITUTED ISOTHIAZOLOPYRIDIN-3(2H)-ONE 1,1-DIOXIDES
Martinez-Merino, Victor,Gil, Maria J.,Zabalsa, Jose M.,Gonzalez, Alberto
, p. 2737 - 2744 (2007/10/03)
The Isothiazolopyridin-3(2H)-one 1,1-dioxides (3a-g) were prepared from the corresponding isothiazolopyridin-3(2H)-ones (1a-g) by means of an oxidation with oxone (KHSO5) and sodium hypochlorite (NaOCl) in two steps.The influen
Heteroaryl-Fused 2-Phenylisothiazolone Inhibitors of Cartilage Breakdown
Wright, Stephen W.,Petraitis, Joseph J.,Abelman, Matthew M.,Batt, Douglas G.,Bostrom, Lori L.,et al.
, p. 3071 - 3078 (2007/10/02)
The synthesis, biological evaluation, and structure-activity relationships of a series of N-phenyl heteroaryl-fused isothiazolones are described.These isothiazolones have been shown to exhibit potent, dose-dependent inhibition of IL-1β-induced breakdown of proteoglycan in a cartilage organ culture assay.This effect is likely due to inhibition of MMP activation and a consequent reduction in MMP activity following IL-1β stimulation.Thus these compounds potentially represent simple, non-peptidic disease-modifying agents for the treatment of arthritic diseases.To examine the effects of structure on in vitro activity, three general features of the molecules were varied, substituents on the pendant N-phenyl group, the position of ring fusion to the isothiazolone, and substituents on the fused ring peri to the isothiazolone sulfur.
