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Synthesis and Antibacterial Evaluation of Novel Vancomycin Derivatives Containing Quaternary Ammonium Moieties.

ABSTRACT: A series of novel vancomycin analogues with quaternary ammonium moieties have been designed and synthesized for fighting with clinically isolated drug-resistant bacteria. Partial target molecules exhibited potent activity against the tested strains. Among all of the compounds, a triazole quaternary ammonium vancomycin (QAV) derivative QAV-a1 exerted the best antibacterial activities. QAV-a1 was found to be 4- to 32-fold more efficacious than vancomycin against MRSA. Meanwhile, QAV-a1 showed a good pharmacokinetic profile with a half-life of 5.19 ± 0.10 h, which is longer than that of vancomycin (4.3 ± 1.9 h). These results provided guidance for the further exploitation of vancomycin derivatives against drug-resistant bacteria.

SUBMITTER: Jiang Y

PROVIDER: S-EPMC10413833 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature

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Synthesis and Antibacterial Evaluation of Novel Vancomycin Derivatives Containing Quaternary Ammonium Moieties.

Jiang Yongwei Y Lin Weixin W Tan Subei S Wang Yuxuan Y Wu Wei W Lu Zhigang Z

ACS omega 20230725 31

A series of novel vancomycin analogues with quaternary ammonium moieties have been designed and synthesized for fighting with clinically isolated drug-resistant bacteria. Partial target molecules exhibited potent activity against the tested strains. Among all of the compounds, a triazole quaternary ammonium vancomycin (QAV) derivative QAV-a1 exerted the best antibacterial activities. QAV-a1 was found to be 4- to 32-fold more efficacious than vancomycin against MRSA. Meanwhile, QAV-a1 showed a go ...[more]

PMID: 37576623

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