The title compounds I [A = alkyl, cyanoalkyl, aryl, etc.; B = absent, O, S, SO, SO2, NH, N(H)​CO; R = (un)​substituted aryl, heteroaryl, heterocycle] and pharmaceutically acceptable salts thereof, able to activate efficaciously the AMPK enzymic complex, and therefore useful in the prophylaxis and therapeutic treatment of diseases and disorders in particular metabolic disorders, such as diabetes and obesity, immune-​mediated inflammatory pathologies and cancer, were prepared and​/or claimed. E.g., a 2-​step synthesis of (2-​(cyanomethyl)​-​1,​3-​dioxoisoindolin-​5-​yl)​benzamide, starting from 5-​aminoisoindoline-​1,​3-​dione and benzoyl chloride, was described. Exemplified compounds I were tested for AMPK activation in the C2C12 cell line (data given)​. Pharmaceutical composition comprising compound I was disclosed.

Preparation of isoindoline derivatives for use as AMPK activators

Antonioli, Luca;Fornai, Matteo;Blandizzi, Corrado;La Motta, Concettina
2018-01-01

Abstract

The title compounds I [A = alkyl, cyanoalkyl, aryl, etc.; B = absent, O, S, SO, SO2, NH, N(H)​CO; R = (un)​substituted aryl, heteroaryl, heterocycle] and pharmaceutically acceptable salts thereof, able to activate efficaciously the AMPK enzymic complex, and therefore useful in the prophylaxis and therapeutic treatment of diseases and disorders in particular metabolic disorders, such as diabetes and obesity, immune-​mediated inflammatory pathologies and cancer, were prepared and​/or claimed. E.g., a 2-​step synthesis of (2-​(cyanomethyl)​-​1,​3-​dioxoisoindolin-​5-​yl)​benzamide, starting from 5-​aminoisoindoline-​1,​3-​dione and benzoyl chloride, was described. Exemplified compounds I were tested for AMPK activation in the C2C12 cell line (data given)​. Pharmaceutical composition comprising compound I was disclosed.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11568/958131
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