Wisconsin Alumni Research Foundation

Gabrielle N Winston-McPherson

Weiping Tang

Xiaoxun Li

Dongxu Shu

Alan D Attie

Mark Patrick Keller

Ka Yang

Haibo Xie

Described are benzoimidazole indolyl methane compounds, pharmaceutical compositions containing them, and use of the compounds to inhibit PCSK9-mediated ailments. The compounds have the structure: 

Benzoimidazole indolyl methanes and methods of using them to inhibit PCKS9 and PCKS9-mediated ailments

Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.

Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them

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Madison, WI, United States of America

Gabrielle N Winston-McPherson