Original articleSynthesis of novel 1,2-benzothiazine 1,1-dioxide-3-ethanone oxime N-aryl acetamide ether derivatives as potent anti-inflammatory agents and inhibitors of monocyte-to-macrophage transformation

Add time:09/04/2019    Source:sciencedirect.com

A series of novel 1,2-benzothiazine 1,1-dioxide-3-ethanone oxime N-aryl acetamide ether derivatives 7a–h and 9a–h were synthesized starting from sodium salt of saccharin 1 in series of steps. Final compounds 7a–h and 9a–h were evaluated for the anti-inflammatory activity and their ability to inhibit monocyte-to-macrophage transformation. Compounds 7e, 9b, 9e and 9h showed impressive anti-inflammatory activities (TNF-α, IL-8 and MCP-1) at micro molar concentration which was found to be better than positive control i.e., piroxicam. Compound 9e marginally and compound 9h significantly inhibited PMA-induced MMP-9 gelatinase activity. Also compounds 9e and 9h greatly inhibited the PMA-induced monocyte-to-macrophage transformation, a pre-requisite step in the formation of atheroma.

We also recommend Trading Suppliers and Manufacturers of 2-amino-1-(2-(trifluoromethyl)phenyl)ethanone hydrochloride (cas 111595-55-2). Pls Click Website Link as below: cas 111595-55-2 suppliers

Prev:Synthesis of novel trifluoromethyl-substituted spiro-[chromeno[4,3-d]pyrimidine-5,1′-cycloalkanes], and evaluation of their analgesic effects in a mouse pain model
Next:Original articleTrifluoromethyl-promoted homocamptothecins: Synthesis and biological activity)