Chapter 3
Single Molecule Non-cleavable Multiply
Active Antibacterials
“Sometimes, less is more.”
—William Shakespeare (attrib.).
Good things come in threes (Latin-“omne trium perfectum”)
Abstract 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.
© The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd. 2021
J. Bremner, Multiple Action-Based Design Approaches to Antibacterials,
https://doi.org/10.1007/978-981-16-0999-2_3
51
Single Molecule Non-cleavable Multiply
Active Antibacterials
“Sometimes, less is more.”
—William Shakespeare (attrib.).
Good things come in threes (Latin-“omne trium perfectum”)
Abstract 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.
© The Author(s), under exclusive license to Springer Nature Singapore Pte Ltd. 2021
J. Bremner, Multiple Action-Based Design Approaches to Antibacterials,
https://doi.org/10.1007/978-981-16-0999-2_3
51