Enzyme inhibitors, their synthesis and methods for use
AssigneesMahmoud H. el Kouni, Fardos N. M. Naguib, F. Schinazi
InventorsMahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
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AssigneesMahmoud H. el Kouni, Fardos N. M. Naguib, F. Schinazi
InventorsMahmoud el Kouni, Fardos N. M. Naguib, Raymond F. Schinazi
Estimating the term…
Novel compounds are provided that are effective to inhibit the activity of DHUDase or UrdPase. Such compounds have the general formula ##STR1## where X is S or Se; Y is I, F, Cl, Br, methoxy, benzyl, selenenylphenyl, or thiophenyl, and R.sub.1 is an acyclo tail having the general formula ##STR2## where R.sub.2 is H, CH.sub.2 OH or CH.sub.2 NH.sub.2 ; R.sub.3 is OH, NH.sub.2, or OCOCH.sub.2 CH.sub.2 CO.sub.2 H; and R.sub.4 is O, S, or CH.sub.2. The compounds can be used in pharmaceutical compositions, along with various chemotherapeutic agents to increase the efficacy of the treatment. These compounds can also be used in methods of treating patients by coadministering or sequentially administering the enzyme inhibiting compounds with a chemotherapeutic agent effective to treat cancers, or viral, fungal, bacterial, or parasitic infections. The compounds have further utility in enhancing imaging. Further, they can be administered alone to prevent and/or treat disorders of pyrimidine catabolism and other physiological disorders.
A compound represented by the formula ##STR7## where X is S or Se;
5-(phenylselenenyl)uracil (PSU).
5-(phenylthio)uracil (PTU).
5-(phenylselenenyl)barbituric acid.
5-(phenylthio)barbituric acid.
A pharmaceutical composition comprising a compound represented by the formula ##STR9## where X is S or Se;
Dependencies are inferred from the claim text.