Zhang, Tian-Yi published the artcileNew ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo, Formula: C17H14F3N3O2S, the publication is Molecular Diversity (2022), 26(2), 1129-1139, database is CAplus and MEDLINE.
In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid I [n = 3; R1 = H, 2-F, 4-Me, 3,4-(CH3)2], II [R2 = H, 3-OMe, 2,4-(CH3)2, 3-CF3, 2,4-Cl2; X = O, NH], III (R3 = Ph, 2,3-dimethoxyphenyl, furan-2-yl, etc.) were designed and synthesized. All compounds have been screened for their anti-inflammatory activity by using an ear edema model. The potent anti-inflammatory compound was subjected to in vitro cyclooxygenase COX-1/COX-2 inhibition assays. In general, the derivatives were found to be potent anti-inflammatory activity. Especially, the compound I (n = 3; R3 = 2,3-dimethoxyphenyl) (IV) exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after i.p. administration, which was better than celecoxib as a pos. control. Mol. docking results unclose the rationale for the interaction of the compound IV with COX-2 enzyme. Further studies revealed that compound IV exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC50) value of 1.16μM and selectivity index (SI = 64.66) value close to that of celecoxib (IC50 = 0.93μM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent.
Molecular Diversity published new progress about 169590-42-5. 169590-42-5 belongs to amides-buliding-blocks, auxiliary class Sulfamide,Immunology/Inflammation,COX, name is 4-(5-(p-Tolyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C10H11NO4, Formula: C17H14F3N3O2S.
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