24683-26-9Relevant articles and documents
5-aminothiazole non-steroidal anti-inflammatory compound as well as preparation method and application thereof
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, (2020/09/20)
The invention discloses a 5-aminothiazole non-steroidal anti-inflammatory compound. The compound which is efficient, low in toxicity and small in side effect is prepared from an ester intermediate containing a thiazine ring and a 5-aminothiazole derivative through a transesterification reaction. The preparation method of the compound is simple, the compound has the active groups of the existing non-steroidal anti-inflammatory medicine; meanwhile, the special change of the nitrogen atom position is also designed; compared with the existing non-steroidal anti-inflammatory medicines, the compoundhas better anti-inflammatory and analgesic effects, particularly has good curative effects on arthritis, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, soft tissue inflammation and thelike, has small toxic and side effects on human bodies, and has a very wide market prospect.
Discovery of cyclicsulfonamide derivatives as 11β-hydroxysteroid dehydrogenase 1 inhibitors
Kim, Se Hoan,Ramu, Ravirala,Kwon, Sung Wook,Lee, Su-Hee,Kim, Chi Hyun,Kang, Seung Kyu,Rhee, Sang Dal,Bae, Myung Ae,Ahn, Sung Hoon,Ha, Duck Chan,Cheon, Hyae Gyeong,Kim, Ki Young,Ahn, Jin Hee
supporting information; experimental part, p. 1065 - 1069 (2010/06/14)
A new series of cyclic sulfonamide derivatives was synthesized and evaluated for their ability to inhibit 11β-HSD1. Cyclic sulfonamides with phenylacetyl substituents at the 2-position showed nanomolar inhibitory activities. Among them, compound 4e exhibited a good in vitro inhibitory activity and selectivity toward human 11β-HSD2.
CONDITIONS OF THE DIECKMANN CONDENSATION OF ALKYL 2-(N-METHYL-N-(ALKOXYCARBONYLMETHYL)SULFAMOYL-BENZOATES
Patek, Marcel,Hampl, Frantisek
, p. 3267 - 3277 (2007/10/02)
The Dieckmann condensation of alkyl 2-(N-methyl-N-(alkoxycarbonylmethyl)sulfamoyl)benzoates IIIa-IIIe with various bases affords alkyl 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylate 1,1-dioxides IVa-IVe which are intermediates in the synthesis of antiinflammatory drug piroxicam.The yields of benzothiazines IVa-IVe depend mostly on the nature of a base, reaction temperature and solvent used for these condensations.Hitherto undescribed esters IIIb-IIIe were sythesized and their structures were confirmed by 1H and 13C NMR, and mass spectra.