203649-58-5

Upstream product

• 203660-02-0 8-chloromethyl-10H-pyrazino[2,3-b][1,4]benzothiazine 
• 741729-98-6 ethyl 4-(piperidin-4-yl)benzoate 
• 203661-96-5 ethyl 4-(1-benzyl-1,2,5,6-tetrahydropyridin-4-yl)benzoate 
• 188863-87-8 1-benzyl-4-(4-bromo-phenyl)-1,2,3,6-tetrahydro-pyridine 

Relevant academic research and scientific papers

Piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4] benzothiazine as orally-active adhesion molecule inhibitors

Novel piperidine carboxylic acid derivatives of 10H-pyrazino[2,3-b][1,4] benzothiazine were prepared and evaluated for their inhibitory activity on the upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1). Replacement of the methanesulfonyl group on the piperidine ring of previously prepared derivatives with a carboxylic acid-containing moiety resulted in a number of potent adhesion molecule inhibitors. Of these, (anti) [3-(10H-pyrazino[2,3-b][1,4]benzothiazin-8-yl)methyl-3-azabicyclo[3.3.1] non-9-yl]acetic acid 2q (ER-49890), showed the most potent oral inhibitory activities against neutrophil migration in an interleukin-1 (IL-1) induced paw inflammation model using mice, and leukocyte accumulation in a carrageenan pleurisy model in the rat, and therapeutic effect on collagen-induced arthritis in rats.