17061-90-4Relevant articles and documents
New ursolic acid derivatives bearing 1,2,3-triazole moieties: design, synthesis and anti-inflammatory activity in vitro and in vivo
Bai, Xue-Qian,Cao, Li-Ting,Li, Chun-Shi,Sun, Si-Mei,Zhang, Tian-Yi,Zhao, Dong-Hai
, (2021/06/07)
Abstract: In order to discover novel anti-inflammatory agents, three series of compounds obtained by appending 1,2,3-triazole moieties on ursolic acid 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 11b exhibited the strongest activity of all of the compounds prepared, with 82.81% inhibition after intraperitoneal administration, which was better than celecoxib as a positive control. Molecular docking results unclose the rationale for the interaction of the compound 11b with COX-2 enzyme. Further studies revealed that compound 11b exhibited effective COX-2 inhibitory activity, with half-maximal inhibitor concentration (IC50) value of 1.16?μM and selectivity index (SI = 64.66) value close to that of celecoxib (IC50 = 0.93?μM, SI = 65.47). Taken together, these results could suggest a promising chemotype for development of new COX-2-targeting anti-inflammatory agent. Graphic abstract: [Figure not available: see fulltext.]
1,2,3-Triazole-based kojic acid analogs as potent tyrosinase inhibitors: Design, synthesis and biological evaluation
Ashooriha, Morteza,Khoshneviszadeh, Mehdi,Khoshneviszadeh, Mahsima,Moradi, Seyed Ershad,Rafiei, Alireza,Kardan, Mostafa,Emami, Saeed
, p. 414 - 422 (2018/11/21)
A series of kojic acid-derived compounds 6a-p bearing aryloxymethyl-1H-1,2,3-triazol-1-yl moiety were designed by modifying primary alcoholic group of kojic acid as tyrosinase inhibitors. The target compounds 6a-p were synthesized via click reaction. All
Bimetal-Catalyzed Cascade Reaction for Efficient Synthesis of N-Isopropenyl 1,2,3-Triazoles via In-Situ Generated 2-Azidopropenes
Liu, Zhenhua,Hao, Wenjing,Liu, Zhixian,Gao, Wen,Zhang, Zhihai,Zhang, Yanan,Li, Xiang,Tong, Lili,Tang, Bo
supporting information, p. 2149 - 2154 (2019/06/13)
A bimetal-catalyzed cascade reaction for the synthesis of N-isopropenyl 1,2,3-triazoles in high yield is reported. This reaction involves the generation of 2-azidopropenes in situ by C(sp3)-OAr bond cleavage for click reaction and features a broad substrate scope, good functional group tolerance and readily available substrates.
