4.5 Conclusion
153
Multi-active
single
molecule
(hybrid) or
molecules
Leads
Prodrug
Combinations
Fig. 4.10 Intersectional diagram for multi-active antibacterial design
There are many possibilities for the design and development of radically new,
triple- or higher action antibacterials from prodrugs and, while the medicinal chemical and other disciplinary challenges are demanding, such antibacterial agents could
ultimately help to meet the antibiotic resistance threat and improve health care
outcomes in the future.
References
Abet V, Filace F, Recio J et al. (2017) Prodrug approach: An overview of recent cases. Eur J Med
Chem 127:810–827
Adjei MD, Heinze TM, Deck J et al. (2006) Transformation of the antibacterial agent norfloxacin
by environmental mycobacteria. Appl Environ Microbiol 72 (9):5790–5793
Allan RN, Kelso MJ, Rineh A et al. (2017) Cephalosporin-NO-donor prodrug PYRRO-C3D shows
β-lactam-mediated activity against Streptococcus pneumoniae biofilms. Nitric Oxide 65:43–49
Anderson SN, Richards JM, Esquer HJ et al. (2015) A structurally-tunable 3-hydroxyflavone motif
for visible light-induced carbon monoxide-releasing molecules. ChemistryOpen 4:590–594
Arrue L, Ratjen L (2017) Internal targeting and external control: phototriggered targeting in
nanomedicine. ChemMedChem 12 (23):1908–1916
Babakhanian M, Yang L, Nowroozi B et al. (2018) Effects of low intensity focused ultrasound on
liposomes containing channel proteins. Sci Rep 8 (1):17250–17250
Baptista PV, McCusker MP, Carvalho A et al. (2018) Nano-strategies to fight multidrug resistant
bacteria-"A Battle of the Titans". Front Microbiol 9:1441–1441
Barraud N, Kardak BG, Yepuri NR et al. (2012) Cephalosporin-3’-diazeniumdiolates: targeted
NO-donor prodrugs for dispersing bacterial biofilms. Angew Chem Int Ed 51 (36):9057–9060
Bartee D, Sanders S, Phillips PD et al. (2019) Enamide prodrugs of acetyl phosphonate deoxy-dxylulose-5-phosphate synthase inhibitors as potent antibacterial agents. ACS infectious diseases
5 (3):406–417
Bio M, Nkepang G, You Y (2012) Click and photo-unclick chemistry of aminoacrylate for visible
light-triggered drug release. Chem Commun 48 (52):6517–6519
153
Multi-active
single
molecule
(hybrid) or
molecules
Leads
Prodrug
Combinations
Fig. 4.10 Intersectional diagram for multi-active antibacterial design
There are many possibilities for the design and development of radically new,
triple- or higher action antibacterials from prodrugs and, while the medicinal chemical and other disciplinary challenges are demanding, such antibacterial agents could
ultimately help to meet the antibiotic resistance threat and improve health care
outcomes in the future.
References
Abet V, Filace F, Recio J et al. (2017) Prodrug approach: An overview of recent cases. Eur J Med
Chem 127:810–827
Adjei MD, Heinze TM, Deck J et al. (2006) Transformation of the antibacterial agent norfloxacin
by environmental mycobacteria. Appl Environ Microbiol 72 (9):5790–5793
Allan RN, Kelso MJ, Rineh A et al. (2017) Cephalosporin-NO-donor prodrug PYRRO-C3D shows
β-lactam-mediated activity against Streptococcus pneumoniae biofilms. Nitric Oxide 65:43–49
Anderson SN, Richards JM, Esquer HJ et al. (2015) A structurally-tunable 3-hydroxyflavone motif
for visible light-induced carbon monoxide-releasing molecules. ChemistryOpen 4:590–594
Arrue L, Ratjen L (2017) Internal targeting and external control: phototriggered targeting in
nanomedicine. ChemMedChem 12 (23):1908–1916
Babakhanian M, Yang L, Nowroozi B et al. (2018) Effects of low intensity focused ultrasound on
liposomes containing channel proteins. Sci Rep 8 (1):17250–17250
Baptista PV, McCusker MP, Carvalho A et al. (2018) Nano-strategies to fight multidrug resistant
bacteria-"A Battle of the Titans". Front Microbiol 9:1441–1441
Barraud N, Kardak BG, Yepuri NR et al. (2012) Cephalosporin-3’-diazeniumdiolates: targeted
NO-donor prodrugs for dispersing bacterial biofilms. Angew Chem Int Ed 51 (36):9057–9060
Bartee D, Sanders S, Phillips PD et al. (2019) Enamide prodrugs of acetyl phosphonate deoxy-dxylulose-5-phosphate synthase inhibitors as potent antibacterial agents. ACS infectious diseases
5 (3):406–417
Bio M, Nkepang G, You Y (2012) Click and photo-unclick chemistry of aminoacrylate for visible
light-triggered drug release. Chem Commun 48 (52):6517–6519