Multiply active non-cleavable antibacterials constitute a complex molecular design area. The emphasis in this chapter is on design parameters for small molecule triple or higher action single agents based on background information from drug combinations and dual action hybrids. Established multiple action agents or multi-targeting of bacterial sites by single ligands are discussed and then new structural possibilities are suggested illustrating the key design principles involved. A feature of this chapter is the use of a known antibacterial, the natural product berberine, as the starting point to illustrate potentially generalizable structural modifications for deliberate multiple action design. Cross referencing to sections of other chapters is included where appropriate. In this chapter there is a concentration on the medicinal chemistry aspects in new antibacterial design.
“Sometimes, less is more.”
—William Shakespeare (attrib.).
Good things come in threes (Latin-“omne trium perfectum”)
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