157672-03-2Relevant academic research and scientific papers
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.
Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
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, (2008/06/13)
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II STR1 wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R3 is selected from lower alkyl and amino; and wherein R4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R1 is not lower alkyl when R3 is methyl and when R4 is hydrido, methyl, methoxy or chloro; or a pharmaceutically-acceptable salt thereof.
