N2,N4-disubstituted pyrimidine-2,4-diamine compounds as antibacterial agents
AssigneeKing Faisal University
InventorsMichelyne Haroun, Christophe Tratrat
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Abstract
The N2,N4-disubstituted pyrimidine-2,4-diamine derivative compounds are antibacterial agents having broad spectrum antibacterial activity. The present N2,N4-disubstituted pyrimidine-2,4-diamine compounds have antimicrobial activity against various susceptible and resistant gram-positive and gram-negative bacteria as well as drug resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Claims9
A compound having the formula I:
- or a pharmaceutically acceptable salt, ester stereoisomer, or solvate thereof, wherein:
- each of X1, X2, X3, and X4 is independently CH or nitrogen, wherein two of X1, X2, and X3, are nitrogen;
- R1 is a C1-C6 alkyl;
- and
- R2, R3 and R5 are each H, R4 is a carboxylic acid, and R6 is (cyclohexyl(methyl))aminomethyl.
A compound having the formula I:
- or a pharmaceutically acceptable salt, ester stereoisomer, or solvate thereof, wherein:
- X1 and X2 are nitrogen;
- X3 is CH;
- X4 is CH or nitrogen;
- R1 is methyl;
- and
- each of R2, R3, and R5 are hydrogen, R4 is a carboxylic acid, and R6 is a (cyclohexyl(methyl)amino)methyl.
A compound selected from the group consisting of:
- 4-((2-((3-acetamidophenyl)amino)pyrimidin-4-yl)amino)-3-((cyclohexyl(methyl)amino)methyl)benzoic acid (7),
- and a pharmaceutically acceptable salt, ester, stereoisomer, or solvate thereof.
Dependencies are inferred from the claim text.