313236-73-6Relevant academic research and scientific papers
Design, synthesis, and biological evaluation of 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) inhibitors
Reddy, M.V. Ramana,Billa, Vinay K.,Pallela, Venkat R.,Mallireddigari, Muralidhar R.,Boominathan, Rengasamy,Gabriel, Jerome L.,Reddy, E. Premkumar
, p. 3907 - 3916 (2008/09/21)
A series of 20 novel 1-(4-sulfamylphenyl)-3-trifluoromethyl-5-indolyl pyrazolines were designed, synthesized, and screened in vitro for anti-inflammatory activity. These compounds were designed for evaluation as dual inhibitors of cyclooxygenases (COX-1 and COX-2) and lipoxygenases (LOX-5, LOX-12, and LOX-15) that are responsible for inflammation and pain. All pyrazoline molecules prepared are optically active and compounds that are more potent in COX-2 inhibitory activity (5a and 5f) were resolved by chiral column and each enantiomer was tested for cyclooxygenase inhibitory activity. Molecular modeling and comparison of molecular models of 5a enantiomers with that of celecoxib model shows that 5a (enantiomer-1) and 5a (enantiomer-2) have more hydrogen bonding interactions in the catalytic domain of COX-2 enzyme than celecoxib. Compounds 5a, 5e, and 5f showed moderate to good LOX-5 and LOX-15 inhibitory activity and this is comparable to that of celecoxib and more potent than rofecoxib.
1-(4-sulfamylaryl)-3-substituted-5-aryl-2-pyrazolines and inhibitors of cyclooxygenase-2
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, (2008/06/13)
Compounds of the formula wherein: X is selected from the group consisting of trihalomethyl, C1-C6alkyl, and a group of formula II: wherein: R3and R4are independently selected from the group consisting of hydroge
