Isoamphipathic antibacterial molecules regulating activity and toxicity through positional isomerism.

ABSTRACT: Peptidomimetic antimicrobials exhibit a selective interaction with bacterial cells over mammalian cells once they have achieved an optimum amphiphilic balance (hydrophobicity/hydrophilicity) in the molecular architecture. To date, hydrophobicity and cationic charge have been considered the crucial parameters to attain such amphiphilic balance. However, optimization of these properties is not enough to circumvent unwanted toxicity towards mammalian cells. Hence, herein, we report new isoamphipathic antibacterial molecules (IAMs: 1-3) where positional isomerism was introduced as one of the guiding factors for molecular design. This class of molecules displayed good (MIC = 1-8 μg mL^-1 or μM) to moderate [MIC = 32-64 μg mL^-1 (32.2-64.4 μM)] antibacterial activity a

SUBMITTER: Barman S 

PROVIDER: S-EPMC10171078 | biostudies-literature | 2023 May

REPOSITORIES: biostudies-literature