40515-19-3Relevant articles and documents
PDGFR kinase inhibitor and use thereof
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Paragraph 0169; 0176-0177, (2021/03/06)
The present invention provides a novel PDGFR kinase inhibitor comprising a compound of formula (I) or a pharmaceutically acceptable salt, solvate, ester, acid, metabolite, or prodrug thereof. The invention also provides a use and a method of the compound of formula (I) for the prevention or treatment of disorders associated with PDGFR kinase activity, in particular for the prevention or treatmentof disorders associated with PDGFR alpha and/or PDGFR beta kinase activity.
New 1,2,3-triazole-based analogues of benznidazole for use against Trypanosoma cruzi infection: In vitro and in vivo evaluations
Leite, Débora Inácio,Fontes, Fábio de Vasconcellos,Bastos, Monica Macedo,Hoelz, Lucas Villas Boas,Bianco, Maria da Concei??o Avelino Dias,de Oliveira, Andressa Paula,da Silva, Patricia Bernardino,da Silva, Cristiane Fran?a,Batista, Denise da Gama Jean,da Gama, Aline Nefertiti Silva,Peres, Raiza Brand?o,Villar, Jose Daniel Figueroa,Soeiro, Maria de Nazaré Correia,Boechat, Nubia
, p. 1670 - 1682 (2018/09/10)
Chagas disease has spread throughout the world mainly because of the migration of infected individuals. In Brazil, only benznidazole (Bnz) is used; however, it is toxic and not active in the chronic phase, and cases of resistance are described. This work aimed at the synthesis and the trypanocidal evaluation in vitro and in vivo of six new Bnz analogues (3–8). They were designed by exploring the bioisosteric substitution between the amide group contained in Bnz and the 1,2,3-triazole ring. All the compounds were synthesized in good yields. With the exception of compound 7, the in vitro biological evaluation shows that all Bnz analogues were active against the amastigote form, whereas only compounds 3, 4, 5, and 8 were active against trypomastigote. Compounds 4 and 5 showed the most promising activities in vitro against the form of trypomastigote, being more active than Bnz. In vivo evaluation of compounds, 3–8 showed lower potency and higher toxicity than Bnz. Although the 1,2,3-triazole ring has been described in the literature as an amide bioisostere, its substitution here has reduced the activity of the compounds and made them more toxic. Thus, further molecular optimization could provide novel therapeutic agents for Chagas’ disease.
Design, synthesis and antifungal activity of novel indole derivatives linked with the 1,2,3-triazole moiety via the CuAAC click reaction
Xu, Guiqing,Zhao, Jinglin,Jiang, Yuqin,Zhang, Peng,Li, Wei
, p. 269 - 272 (2016/07/06)
A series of novel indole derivatives linked with the 1,2,3-triazole moiety was designed, synthesised by the CuCl2/Zn-catalysed Huisgen cycloaddition and characterised. The antifungal activity of all the prepared compounds against Colletotrichum capsici and cotton Physalospora pathogens was evaluated and the results indicated that these compounds showed inhibitory effect for fungi and the inhibition ratio of the best was up to 83.3%. The preliminary structure-activity relationship is also discussed in this paper.