33512-71-9Relevant articles and documents
Emergent antibacterial activity ofN-(thiazol-2-yl)benzenesulfonamides in conjunction with cell-penetrating octaarginine
Das Mahapatra, Amarjyoti,Datta, Bhaskar,Hadianawala, Murtuza,Majhi, Sasmita,Mishra, Abhijit,Pandit, Shiny,Ratrey, Poonam
, p. 28581 - 28592 (2021/09/22)
Hybrid antimicrobials that combine the effect of two or more agents represent a promising antibacterial therapeutic strategy. In this work, we have synthesizedN-(4-(4-(methylsulfonyl)phenyl)-5-phenylthiazol-2-yl)benzenesulfonamide derivatives that combine
Synthesis and biological evaluation of 2-trifluoromethyl/sulfonamido-5,6-diaryl substituted imidazo[2,1-b]-1,3,4-thiadiazoles: A novel class of cyclooxygenase-2 inhibitors
Gadad, Andanappa K.,Palkar, Mahesh B.,Anand,Noolvi, Malleshappa N.,Boreddy, Thippeswamy S.,Wagwade
, p. 276 - 283 (2008/03/28)
A series of 2-trifluoromethyl/sulfonamido-5,6-diarylsubstituted imidazo[2,1-b]-1,3,4-thiadiazole derivatives 15a-j have been synthesized by the reaction of 2-amino-5-trifluoromethyl/sulfonamido-1,3,4-thiadiazoles 14a-b and appropriately substituted α-bromo-1,2-(p-substituted)diaryl-1-ethanones 13a-h. Structures of these compounds were established by IR, 1H NMR, 13C NMR, Mass, and HRMS data. The selected compounds were evaluated for their preliminary in vitro cyclooxygenase inhibitory activity against COX-2 and COX-1enzymes using colorimetric method. The compounds tested showed selective inhibitory activity toward COX-2 (80.6-49.4%) over COX-1 (30.6-8.6), amongst them compounds 15f and 15j showed appreciable COX-2 selective inhibitory activity. These compounds also exhibited significant anti-inflammatory activity (70.09-42.32%), which is comparable to that of celecoxib in the carrageenan-induced rat paw edema method.
Synthesis and biological evaluation of 2,3-diarylpyrazines and quinoxalines as selective COX-2 inhibitors
Singh, Sunil K.,Saibaba,Ravikumar,Rudrawar, Santosh V.,Daga, Pankaj,Rao, C. Seshagiri,Akhila,Hegde,Rao, Y. Koteswar
, p. 1881 - 1893 (2007/10/03)
Several 2,3-diaryl pyrazines and quinoxalines with 4-sulfamoyl (SO 2NH2)/methylsulfonyl (SO2Me)-phenyl pharmacophores have been synthesized and evaluated for the cyclooxygenase (COX-1/COX-2) inhibitory activity. Smaller groups such as methoxy, methyl and fluoro when substituted at/around position-4 of the adjacent phenyl ring, have great impact on the selective COX-2 inhibitory activity of the series. Many potential compounds were obtained from a brief structure-activity relationship (SAR) study. Two of these, compounds 11 and 25 exhibited excellent in vivo activity in the established animal model of inflammation. Since compound 25 possessed an amenable sulfonamide group, two of its prodrugs 48 and 49 were also synthesized. Both of them have excellent in vivo potential, and represent a new class of COX-2 inhibitor.