1. Two different pharmacophoric domains attached covalently by a linker domain.
Two different pharmacophoric domains attached covalently by a linker domain. The lability of the linker determines the type of antibiotic hybrid generated. A linker that can be enzymatically degraded (preferably by only bacterium-specific enzymes) gives rise to two functional pharmacophoric entities that are thus used in the antibiotic hybrid prodrug strategy. A linker that is inert to enzymatic degradation is used to hold the two pharmacophoric domains together in the antibiotic hybrid drug strategy.
Ronald Domalaon et al. Clin. Microbiol. Rev. 2018; doi: /CMR