Medical University of South Carolina

North Carolina State University

Edward D'Antonio

Joshua G Pierce

Jennifer D'Antonio

One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such asribose 5-phosphate isomerase type B and D-ribulose-5-phosphate 3-epimerase enzymes. Methods can be used in forming pharmaceutical compositions for use in treatment of disease caused by kinetoplastid parasites including, andspp.

One-step synthesis of phosphate-based inhibitors and applications thereof

Inhibitor compounds with biological activity against kinetoplastid parasites, along with methods of use of the compounds, are provided. The compounds can be used to strongly inhibit key drug targets found in protozoan parasites, e.g., the targetglucokinase. Compounds include derivatives of 3-nitro-2-phenyl-2H-chromene, and monosaccharide amines including D-glucosamine, D-mannosamine, D-galactosamine, and D-fructosamine.

Monosaccharide amine and 3-nitro-2-phenyl-2H-chromene based inhibitors of glucose kinases

Compounds discovered through a high-throughput screen, along with methods of use of the compounds, are provided. The compounds can be used to strongly inhibit key drug targets found in protozoan parasites, e.g., the targetglucokinase. Compounds include derivatives of N-phenylbenzenesulfonamide, barbituric acid, (R)-3-(piperidin-2-yl)pyridine, 3-nitro-2-phenyl-2H-chromene, 6-amino-3-methyl-4-phenyl-1,4-dihydropryranole[2,3-c]pyrazole-5-carbonitrile, and gossypol (2,2'-Bis(formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene).

Inhibitors of glucose kinases, along with methods of their formation and use

Compounds are generally provided, along with pharmaceutical compositions including such compounds. Methods are also generally provided for inhibiting ribose 5-phosphate isomerase in a human, such as via administering to the human the pharmaceutical composition that includes such a compound. Methods are also generally provided for treating a mammal that is infected by a parasitic organism, such as via administering to the mammal the pharmaceutical composition that includes such a compound. Methods are also generally provided for forming a pharmaceutical composition.

Cysteine-modifying substrate analogue inhibitors of ribose 5-phosphate isomerase for parasitic diseases, along with methods of their formation and use

Methods for treating a mammal that is infected by a parasitic organism are provided, along with pharmaceutical compositions and compounds. The method includes administering to the mammal the pharmaceutical composition of FIG., where: R, R, R, and Rcomprises, independently, H, OH, NH, SH, a halogen, or an organic group or a derivative thereof; Xis O, NH, CH, or S; m is 0 or 1; Xcomprises an organic linkage, such as CH; n is an integer from 0 to 10; and Rcomprises an aromatic organic group.

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Bluffton, SC, United States of America

Edward D'Antonio