The invention is related to boronate compds. of formula I with neuroprotective, antiplatelet, antitumor, and antimicrobial activities for the treatment of diseases and conditions assocd. to oxidative stress. Compds. of formula I wherein X1 and X2 are independently CH and CH2; X3 and X4 are independently S and SH; A is (CH2)​n; n is 1 to 10; R is H, (un)​substituted alkyl, (un)​substituted aryl, etc.; R1 and R2 are independently H, CH3, alkyl, etc.; R1 and R2 can be taken together to in a cyclic compd.; and their pharmaceutically acceptable stereoisomers, enantiomers, conformers and racemic mixt. of different stereoisomers thereof, are claimed. Example compd. II was prepd. by amidation of 5-​(S)​-​(1,​2-​dithiolanyl-​3-​yl)​pentanoic acid with 3a,​5,​5-​trimethylhexahydro-​4,​6-​methanobenzo[d]​[1,​3,​2]​dioxaborol-​2-​ylmethylamine hydrochloride. The compds. of formula I were evaluated for their antiplatelet activity (data given)​.

Preparation of boronate derivatives for the treatment of diseases and conditions associated to oxidative stress

DI STEFANO ANTONIO;CACCIATORE IVANA;
2018

Abstract

The invention is related to boronate compds. of formula I with neuroprotective, antiplatelet, antitumor, and antimicrobial activities for the treatment of diseases and conditions assocd. to oxidative stress. Compds. of formula I wherein X1 and X2 are independently CH and CH2; X3 and X4 are independently S and SH; A is (CH2)​n; n is 1 to 10; R is H, (un)​substituted alkyl, (un)​substituted aryl, etc.; R1 and R2 are independently H, CH3, alkyl, etc.; R1 and R2 can be taken together to in a cyclic compd.; and their pharmaceutically acceptable stereoisomers, enantiomers, conformers and racemic mixt. of different stereoisomers thereof, are claimed. Example compd. II was prepd. by amidation of 5-​(S)​-​(1,​2-​dithiolanyl-​3-​yl)​pentanoic acid with 3a,​5,​5-​trimethylhexahydro-​4,​6-​methanobenzo[d]​[1,​3,​2]​dioxaborol-​2-​ylmethylamine hydrochloride. The compds. of formula I were evaluated for their antiplatelet activity (data given)​.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11564/704879
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