19155-93-2Relevant articles and documents
Arylethenylbenzofuroxan derivatives as drugs for chagas disease: Multigram batch synthesis ysubg a wuttug#bideb process
Porcal, Williams,Merlino, Alicia,Boiani, Mariana,Gerpe, Alejandra,Gonzalez, Mercedes,Cerecetto, Hugo
, p. 156 - 162 (2008)
In the present work, we developed robust processes for the preparation of new antitrypanosomal benzofuroxans, E and Z isomers of 5-arylethenylbenzo[1,2-c] 1,2,5-oxadiazole p1N-oxide 1-6, in muhigram batch through Wittig-Boden conditions as the key synthetic step. In these conditions, the generation of the benzofurazans, as secondary byproduct, was minimized.
Piperidine compound and preparation method and medical application thereof
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Paragraph 0589-0591; 0593, (2021/04/07)
The invention discloses a piperidine compound shown as a formula (I) and a preparation method and medical application thereof, and particularly relates to a piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof and a preparation method and application of the piperidine USP7 inhibitor compound or pharmaceutically acceptable salt or ester or solvate thereof. The compound provided by the invention can inhibit the activity of USP7 enzyme, has very good selectivity and druggability, and can be used for preparing medicines for preventing or treating tumor diseases or virus infectious diseases.
Design, synthesis and biological evaluation of N-oxide derivatives with potent in vivo antileishmanial activity
da Costa Clementino, Leandro,Fernandes, Guilherme Felipe Santos,Prokopczyk, Igor Muccilo,Laurindo, Wilquer Castro,Toyama, Danyelle,Motta, Bruno Pereira,Baviera, Amanda Martins,Henrique-Silva, Flávio,dos Santos, Jean Leandro,Graminha, Marcia A.S.
, (2021/11/08)
Leishmaniasis is a neglected disease that affects 12 million people living mainly in developing countries. Herein, 24 new N-oxide-containing compounds were synthesized followed by in vitro and in vivo evaluation of their antileishmanial activity. Compound 4f, a furoxan derivative, was particularly remarkable in this regard, with EC50 value of 3.6 μM against L. infantum amastigote forms and CC50 value superior to 500 μM against murine peritoneal macrophages. In vitro studies suggested that 4f may act by a dual effect, by releasing nitric oxide after biotransformation and by inhibiting cysteine protease CPB (IC50: 4.5 μM). In vivo studies using an acute model of infection showed that compound 4f at 7.7 mg/Kg reduced ~90% of parasite burden in the liver and spleen of L. infantum-infected BALB/c mice. Altogether, these outcomes highlight furoxan 4f as a promising compound for further evaluation as an antileishmanial agent.
SNAr azidation of phenolic functions utilizing diphenyl phosphorazidate
Ishihara, Kotaro,Shioiri, Takayuki,Matsugi, Masato
supporting information, (2019/12/27)
A useful method for the synthesis of aryl azides via SNAr reaction of phenol derivatives using diphenyl phosphorazidate (DPPA) as an azidation reagent was developed. Various phenol derivatives bearing electron-withdrawing groups were converted into the corresponding aryl azides in a single step. This method is easy to perform and enables the preparation of aryl azides without the use of explosive azide sources.
