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Novel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential.

ABSTRACT: We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-negative and Gram-positive bacteria. They could compromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in the MRSA-infected thigh burden mouse model.

SUBMITTER: Teng P

PROVIDER: S-EPMC5690803 | biostudies-literature | 2017 Oct

REPOSITORIES: biostudies-literature

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Novel bis-cyclic guanidines as potent membrane-active antibacterial agents with therapeutic potential.

Teng Peng P Nimmagadda Alekhya A Su Ma M Hong Yuzhu Y Shen Ning N Li Chunpu C Tsai Ling-Yu LY Cao Jessica J Li Qi Q Cai Jianfeng J

Chemical communications (Cambridge, England) 20171001 87

We designed a class of small dimeric cyclic guanidine derivatives which display potent antibacterial activity against both multidrug-resistant Gram-negative and Gram-positive bacteria. They could compromise bacterial membranes without developing resistance, inhibit biofilms formed by E. coli, and exhibit excellent in vivo activity in the MRSA-infected thigh burden mouse model. ...[more]

PMID: 29052670

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