The University of North Carolina at Chapel Hill

North Carolina Central University

Albert Einstein College of Medicine

John Scott

Matthew Robert Redinbo

Li-An Yeh

Alfred L Williams

Sridhar Mani

Bret David Wallace

Kimberly Terry Lane

This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.

Phenoxy thiophene sulfonamides and their use as inhibitors of glucuronidase

Compounds, compositions and methods are provided that comprise selective &#x3b2;-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial &#x3b2;-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial &#x3b2;-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.

Selective beta-glucuronidase inhibitors as a treatment for side effects of camptothecin antineoplastic agents

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Durham, NC, United States of America

John Scott