Preliminary SAR of Novel Pleuromutilin-Polyamine Conjugates.

ABSTRACT: While pleuromutilin (1) and its clinically available derivatives (2-6) are highly effective against Gram-positive bacteria, they remain inactive against many pathogenic Gram-negative bacteria due to the efflux pump AcrAB-TolC. In an effort to broaden the spectrum of activity of pleuromutilin (1), we developed a series of novel pleuromutilin-polyamine conjugates (9a-f) which exhibited promising intrinsic antimicrobial properties, targeting both Gram-positive and Gram-negative bacteria, including Staphylococcus aureus, methicillin-resistant S. aureus (MRSA), and Escherichia coli, along with the fungal strain Cryptococcus neoformans, and were devoid of cytotoxic and hemolytic properties with the exception of one conjugate.

SUBMITTER: Sue K 

PROVIDER: S-EPMC10673369 | biostudies-literature | 2023 Nov

REPOSITORIES: biostudies-literature