Convenient synthesis of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides

Abstract

Abstract:

A series of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides have been obtained by modification of neamine (1), kanamycin (2) and ribostamycin (3) at 1, 6' and 3'' N-sites, respectively, through selective cyclization and nucleophilic ring-opening of cyclic carbamates. All the products showed no noticeable activity in the antibiotic test in vitro. The result suggests that the urea-linked hydroxyl-alkylamine derivatives of aminoglycosides may not be suitable structures for the enhancement of antibiotic activity.

Key words: Aminoglycoside, Aminoglycoside, Hydroxyl-alkylamine derivative, Hydroxyl-alkylamine derivative, Synthesis, Synthesis, Antibiotic activity, Antibiotic activity

CLC Number:

R931.5

Supporting:

Pan Pan, Gui-Hui Chen, Xiang-Bao Meng, Ying Chen , Zhong-Jun Li^*, Shu-Chun Li^*. Convenient synthesis of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides [J]. .

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Convenient synthesis of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides

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