86601-34-5Relevant academic research and scientific papers
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1
Al-Mourabit, Ali,Bach, Stéphane,Baratte, Blandine,Benchekroun, Mohamed,Delehouzé, Claire,Ermolenko, Ludmila,Iorga, Bogdan I.,Josselin, Béatrice,Nedev, Hristo,Ruchaud, Sandrine,Souab, Mohamed,Tran, Minh Quan,Vagneux, Agathe
, (2020)
With the aim to develop new chemical tools based on simplified natural metabolites to help deciphering the molecular mechanism of necroptosis, simplified benzazole fragments including 2-aminobenzimidazole and the 2-aminobenzothiazole analogs were prepared during the synthesis of the marine benzosceptrin B. Conpounds inhibiting the RIPK1 protein kinase were discovered. A library of 54 synthetic analogs were prepared and evaluated through a phenotypic screen using the inhibition of the necrotic cell death induced by TNF-α in human Jurkat T cells deficient for the FADD protein. This article reports the design, synthesis and biological evaluation of a series of 2-aminobenzazoles on the necroptotic cell death through the inhibition of RIPK1 protein kinase. The 2-aminobenzimidazole and 2-aminobenzothiazole platforms presented herein can serve as novel chemical tools to study the molecular regulation of necroptosis and further develop lead drug candidates for chronic pathologies involving necroptosis.
Phosphonium-mediated cyclization of N-(2-aminophenyl)thioureas: Efficient synthesis of 2-aminobenzimidazoles
Wan, Zhao-Kui,Ousman, Erena Farah,Papaioannou, Nikolaos,Saiah, Eddine
supporting information; experimental part, p. 4149 - 4152 (2011/09/19)
BOP efficiently promoted the phosphonium-mediated cyclization of thioureas, leading to a convenient synthesis of 2-aminobenzimidazoles. Compared to conventional methods, the reactions were complete at room temperature with times ranging from a few minutes
Dithiocarbamate and CuO promoted one-pot synthesis of 2-(N-substituted)-aminobenzimidazoles and related heterocycles
Das, Parthasarathi,Kumar, C. Kiran,Kumar, K. Naresh,Innus,Iqbal, Javed,Srinivas, Nanduri
, p. 992 - 995 (2008/09/17)
A rapid and efficient one-pot method for the synthesis of 2-(N-substituted)-aminobenzimidazoles is described. The reaction is promoted by dithiocarbamate and catalytic CuO. This procedure is general and can be applied to synthesize many potential drug can
