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Macrocycles antibacterial amine.

2003 
Compound of formula (See formula) wherein R1 is hydrogen, C1-C6 alkyl, C6-C10 aryl, 5- to 10-membered, 4- to 10-membered, alkyl C1-C6-alkoxycarbonyl, aryl- C6-C10-carbonyl, heterocyclylcarbonyl 4 to 10 members, heteroarylcarbonyl of 5 to 10 members, alkoxy-C1-C6-alkoxycarbonyl, aminocarbonyl, C1-C6-alkylaminocarbonyl, di-C1-C6-alkylaminocarbonyl, alkyl C1- C6-alkylsulfonyl, aryl-C6-C10-alkylsulfonyl, heterocyclylsulfonyl 4 to 10 membered heteroarylsulfonyl 5 to 10 members or a residue of alpha-amino acid in the L or D configuration bonded via the carbonyl group of the acid function of the amino acid , R1 may be substituted, except hydrogen, with 0, 1, 2 or 3 substituents R1-1 and R1-1 substituents being selected independently from the group consisting of halogen, C1-C6 alkyl, trifluoromethyl, trifluoromethoxy, nitro, cyano, amino, alkyl-C1-C6-alkylamino, di-C1-C6-alkylamino, C3-C8 cycloaliphatic, C6 C10, 5- to 10-membered, 4- to 10-membered, hydroxy, C1-C6 and carboxyl, R2 is hydrogen or C1-C6alkyl, R2 may be substituted, except hydrogen, with 0 , 1, 2 or 3 substituents R2-1 and R2-1 substituents being selected independently from the group consisting of halogen, amino, alkyl-C1-C6-alkylamino and di-C1-C6 alkyl amino, or R1 and R2 form, together with the nitrogen atom to which they are attached, a 4- to 10-membered may be substituted with 0, 1 or 2 substituents R1-2, R1-2 substituents being selected independently from the group consisting of halogen, trifluoromethyl, amino, alkyl C1-C6-alkylamino, di-C1-C6-alkylamino, C3-C8 cycloalkyl, C6-C10 aryl, 5- to 10-membered, 4- to 10-membered, hydroxy, C1-C6 alkoxy, carboxy alkoxy-C1-C6-alkoxycarbonyl and aminocarbonyl, R3 is hydrogen, C1-C6 alkyl or the alpha-amino side group of a presen like in nature in the L or D configuration, loscuales alkyl may be substituted with 0, 1, 2 or 3 substituents R3-1, R3-1 substituents being selected independently from the group consisting of trifluoromethyl, nitro, amino, -C1-C6-alkylamino, di-C1-C6-alkylamino, C3-C8 cycloalkyl, C6-C10 aryl, 5- to 10-membered, 4- to 10-membered, hydroxy, C1-C6 alkoxy, carboxyl, alkoxy- C1-C6-alkoxycarbonyl, aminocarbonyl, C1-C6-alkylaminocarbonyl, di-C1-C6-alkylaminocarbonyl, guanidino and amidino, of which cycloalkyl, aryl, heteroaryl and heterocyclyl may be substituted with 0, 1 or 2 substituents R3- 2 substituents R3-2 being selected independently from the group consisting of halogen, C1-C6, trifluoromethyl and amino alkyl; or a salt thereof, its solvates or the solvates of its salts.
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