161448-78-8Relevant articles and documents
Synthesis of novel dihydronaphthothiazine S,S-dioxides by intramolecular sulfonylamidomethylation of 2-naphthylmethanesulfonamides using Amberlyst XN-1010
Sasiambarrena, Leandro D.,Cánepa, Alicia S.,Bravo, Rodolfo D.
, p. 7184 - 7189 (2015)
We describe herein an efficient synthetic method for novel dihydronaphthothiazines S,S-dioxides by aromatic intramolecular sulfonylamidomethylation of 2-naphthylmethanesulfonamides with s-trioxane using Amberlyst XN-1010 as acid heterogeneous catalyst. Cyclization of the formed sulfonyliminium ion occurred with high regioselectivity and in excellent yields.
Designing anti-inflammatory drugs from parasitic worms: A synthetic small molecule analogue of the acanthocheilonema viteae product ES-62 prevents development of collagen-induced arthritis
Al-Riyami, Lamyaa,Pineda, Miguel A.,Rzepecka, Justyna,Huggan, Judith K.,Khalaf, Abedawn I.,Suckling, Colin J.,Scott, Fraser J.,Rodgers, David T.,Harnett, Margaret M.,Harnett, William
, p. 9982 - 10002 (2014/01/17)
In spite of increasing evidence that parasitic worms may protect humans from developing allergic and autoimmune diseases and the continuing identification of defined helminth-derived immunomodulatory molecules, to date no new anti-inflammatory drugs have been developed from these organisms. We have approached this matter in a novel manner by synthesizing a library of drug-like small molecules based upon phosphorylcholine, the active moiety of the anti-inflammatory Acanthocheilonema viteae product, ES-62, which as an immunogenic protein is unsuitable for use as a drug. Following preliminary in vitro screening for inhibitory effects on relevant macrophage cytokine responses, a sulfone-containing phosphorylcholine analogue (11a) was selected for testing in an in vivo model of inflammation, collagen-induced arthritis (CIA). Testing revealed that 11a was as effective as ES-62 in protecting DBA/1 mice from developing CIA and mirrored its mechanism of action in downregulating the TLR/IL-1R transducer, MyD88. 11a is thus a novel prototype for anti-inflammatory drug development.
Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
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Page/Page column 15, (2010/11/29)
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.