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Optimized versions of an antimalarial chemotype

详细技术说明

Novel classes of compounds which have useful carboxylesterase inhibitory activity are provided, including both generic inhibitors, as well as compounds selective for the human intestinal carboxylester

*Abstract

Novel classes of compounds which have useful carboxylesterase inhibitory activity are provided, including both generic inhibitors, as well as compounds selective for the human intestinal carboxylesterase. These compounds can be used to treat or ameliorate the toxic effects of cancer therapy drugs (such as CPT-11), the effects of the drug overdose, or to increase the efficacy of existing insecticides and pesticides. Granted Patents or Published Applications US 7,973,034 Related Scientific References Wadkins, R.M. et al., "Discovery of Novel Selective Inhibitors of Human Intestinal Carboxylesterase for the Amelioration of Irinotecan-Induced Diarrhea: Synthesis, Quantitative Structure-Activity Relationship Analysis, and Biological Activity", Molecular Pharmacology 65(6): 1336-1342 (June 2004)Wadkins R.M., et al., "Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases." Journal of Medicinal Chemistry 48:2906-2915, 2005. Licensing Opportunities We are currently seeking licensing opportunities in all fields for the development of this technology. Contact the Office of Technology Licensing (Phone: 901-595-2342, Fax: 901-595-3148) for more information.

国家/地区

美国