摘要:
The invention relates to D-Ala-D-Ala ligase inhibitors having the formula: wherein R1 is NH2; R2 is NH2; R3 is selected from hydrogen, alkyl, amino, hydroxy, alkoxy, and alkylamino; and R4 and R4′ are each independently hydrogen or a substituted or unsubstituted, linear, branched, or cyclic, alkyl, alkenyl, alkynyl, aryl, acyl, aralkyl, or alkaryl group wherein one or more carbon or hydrogen atoms may be substituted by a substituent selected from amino, alkylamino, hydroxyl, alkoxyl, thio, halogen, nitro, and carbonyl; wherein NR4R4′ incorporates a substituted or unsubstituted naphthyl group, wherein the substituents are selected from alkoxy, halogen, alkyl, and alkylene, and wherein said naphthyl group in NR4R4′ is bonded to N through a substituted or unsubstituted alkylene moiety. These compounds have antibacterial properties based on their ability to bind and inhibit D-Ala-D-Ala ligase, a critical pathway enzyme in bacterial cell-wall synthesis, and are suitable for various antibacterial uses.
摘要翻译:本发明涉及具有下式的D-Ala-D-Ala连接酶抑制剂:其中R 1是NH 2; R 2是NH 2; R 3选自氢,烷基,氨基,羟基,烷氧基和烷基氨基; 和R 4和R 4'各自独立地为氢或取代或未取代的直链,支链或环状的烷基,烯基,炔基,芳基,酰基,芳烷基, 或烷芳基,其中一个或多个碳原子或氢原子可以被选自氨基,烷基氨基,羟基,烷氧基,硫代,卤素,硝基和羰基的取代基取代; 其中NR 4 R 4'含有取代或未取代的萘基,其中取代基选自烷氧基,卤素,烷基和亚烷基,并且其中NR中的所述萘基 4“4”通过取代或未取代的亚烷基部分与N键合。 这些化合物基于其结合和抑制细菌细胞壁合成中的关键途径酶D-Ala-D-Ala连接酶的能力而具有抗菌特性,并且适用于各种抗菌用途。