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US 2011/0218220 A1Published application
Rationally improved isoniazid and ethionamide derivatives and activity through selective isotopic substitution
AssigneesStc.Unm, The John Hopkins University
InventorsGraham Timmins, Sharon Master, Vojo P. Deretic, William Bishai
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Abstract
The present invention relates to the use of isotopically labeled derivatives of isoniazid, ethionamide and related compounds as effective therapy for the treatment of mycobacterial diseases, including Mycobacterium tuberculosis.
Claims44
A compound according to the chemical structure:
- Where X is an oxygen or a sulfur atom selected from the group consisting of 16O, 17O, 18O, 32S, 33S and 34S;
- Y is a carbon atom selected from the group consisting of 12C and 13C;
- Z is a NH2 group or a NHNH2 group, which group is optionally isotopically labeled with at least one 15N atom;
- R is H or a C1-C3 alkyl group, with the proviso that R is H and Z is an optionally isotopically labeled NHNH2 group when X is an oxygen atom and R is a C1-C3 alkyl group, preferably an ethyl group and Z is an optionally isotopically labeled NH2 group when X is a sulfur atom;
- Wherein at least one of X, Y and Z is isotopically labeled, or
- a pharmaceutically acceptable salt thereof.
3 more elements
Dependencies are inferred from the claim text.