| 摘要 |
The present invention concerns compounds of general formula (I):;;in which Y and Z are chosen from CH and N; T is chosen from CO or SO2; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway |
| 主权项 |
1. A method of treatment of bacterial and mycobacterial infection comprising administering, to a patient in need thereof, an effective amount of a compound of general formula (I):in which
Y and Z are chosen, independently from one another, from CH and N; T is chosen from CO or SO2; n is an integer greater than or equal to 1 and lower than or equal to 3; R1 represents a group chosen from linear or branched C1-C3 alkyl chains, linear or branched and substituted C1-C3 alkyl chains, C3-C6 cyclic groups, the cyano group, the azido group, C1-C3 alkoxy chains, an unsubstituted phenyl group, a phenyl group substituted by one, two or three substituents chosen, independently from one another, from linear or branched C1-C3 alkyl chains, trifluoromethyl, linear or branched C1-3 alkoxy chains, halogens, 6-membered heterocycles comprising 1 or 2 nitrogen atoms in the ring; aromatic 5-membered heterocycles; R is chosen from the azido, cyano, 2-benzothiazolyl groups and the following groups (R-1) to (R-10):in which:
R2 is chosen from H, F, Cl, Br, I; R3 is a group chosen from H, linear or branched C1-C6 alkyl chains, linear or branched C1-C6 alkyl chains substituted by at least one fluorine atom, C3-C6 cyclic groups, the cyanomethyl group, the azidomethyl group, linear or branched C1-C4 alkoxy chains, C1-C4 hydroxyalkyl groups, C1-C4 alkyl methyl ester groups, C1-C4 methylcarbonylamino alkyl groups, C1-C4 methylsulfone alkyl groups, the unsubstituted phenyl group, a phenyl group substituted by one, two or three substituents chosen, independently from one another, from C1-C3 alkyl chains, trifluoromethyl, C1-3 alkoxy chains, optionally substituted aromatic heterocycles, substituted aromatic heterocycles, aromatic heterocycles substituted by at least one fluorine atom or by a group chosen among the following groups (II-a and II-b):in which
R4 is a group chosen from H, linear or branched C1-C4 alkyl chains, the phenyl group, a phenyl group substituted by at least one halogen atom, a phenyl group substituted by a linear or branched C1-C4 alkyl chain, a phenyl group substituted by a linear or branched C1-C4 alkoxy chain and a phenyl group substituted by a trifluoromethyl group. |
