116
3 Single Molecule Non-cleavable Multiply Active Antibacterials
Naruto S, Mizuta H, Nishimura H (1976) A novel amination of isoquinolinium salts via nucleophilic
substitution reaction. Tetrahedron Lett 17 (19):1597–1600
Nasr T, Bondock S, Ibrahim TM et al. (2020) New acrylamide-sulfisoxazole conjugates as
dihydropteroate synthase inhibitors. Bioorg Med Chem 28 (9):115444
Nechepurenko IV, Salakhutdinov NF, Tolstikov GA (2010) Berberine chemistry and biological
activity. Chem Sustain Dev 18:1–23
Okano A, Isley N, Boger D (2017) Peripheral modifications of [[CH 2 NH]Tpg 4] vancomycin
with added synergistic mechanisms of action provide durable and potent antibiotics. Proc Natl
Acad Sci U.S.A. 114:201704125
Oldfield E, Feng X (2014) Resistance-resistant antibiotics. Trends Pharmacol Sci 35 (12):664–674
Olleik H, Yacoub T, Hoffer L et al. (2020) Synthesis and evaluation of the antibacterial activities
of 13-substituted berberine derivatives. Antibiotics 9 (7):381
Opperman TJ, Nguyen ST (2015) Recent advances toward a molecular mechanism of efflux pump
inhibition. Front Microbiol 6: Article 421
Owens B (2017) Solithromycin rejection chills antibiotic sector. Nat Biotechnol 35 (3):187–188
Ozçelik B, Kartal M, Orhan I (2011) Cytotoxicity, antiviral and antimicrobial activities of alkaloids,
flavonoids, and phenolic acids. Pharm Biol 49 (4):396–402
Park KD, Lee JH, Kim SH et al. (2006) Synthesis of 13-(substituted benzyl) berberine and
berberrubine derivatives as antifungal agents. Bioorg Med Chem Lett 16 (15):3913–3916
Parker EN, Drown BS, Geddes EJ et al. (2020) Implementation of permeation rules leads to a FabI
inhibitor with activity against Gram-negative pathogens. Nat Microbiol 5 (1):67–75
Parkes AL, Yule IA (2016) Hybrid antibiotics - clinical progress and novel designs. Expert Opin
Drug Discov 11 (7):665–680
Parmar A, Iyer A, Lloyd DG et al. (2017) Syntheses of potent teixobactin analogues against
methicillin-resistant Staphylococcus aureus (MRSA) through the replacement of l-alloenduracididine with its isosteres. Chem Commun 53 (55):7788–7791
Peek J, Lilic M, Montiel D et al. (2018) Rifamycin congeners kanglemycins are active against
rifampicin-resistant bacteria via a distinct mechanism. Nat Commun 9 (1):4147
Peek J, Xu J, Wang H et al. (2020) A semisynthetic Kanglemycin shows in vivo efficacy against
high-burden rifampicin resistant pathogens. ACS Infect Dis 6:2431–2440
Peterson RM, Huang T, Rudolf JD et al. (2014) Mechanisms of self-resistance in the platensimycinand platencin-producing Streptomyces platensis MA7327 and MA7339 strains. Chem Biol 21
(3):389–397
Pitts CR, Bornemann D, Liebing P et al. (2019) Making the SF 5 group more accessible: A gasreagent-free approach to aryl tetrafluoro-λ 6 -sulfanyl chlorides. Angew Chem Int Ed 58:1950–
1954
Pokrovskaya V, Baasov T (2010) Dual-acting hybrid antibiotics: a promising strategy to combat
bacterial resistance. Expert Opin Drug Discov 5 (9):883–902
Rajendran L, Knölker HJ, Simons K (2010) Subcellular targeting strategies for drug design and
delivery. Nat Rev Drug Discov 9 (1):29–42
Ramesh R, Reddy DS (2018) Quest for novel chemical entities through incorporation of silicon in
drug scaffolds. J Med Chem 61 (9):3779–3798
Richter MF, Drown BS, Riley AP et al. (2017) Predictive compound accumulation rules yield a
broad-spectrum antibiotic. Nature 545 (7654):299–304
Roselli M, Cavalluzzi MM, Bruno C et al. (2016) Synthesis and evaluation of berberine derivatives
and analogs as potential antiacetylcholinesterase and antioxidant agents. Phytochem Lett 18:150–
156
Rzhepishevska O, Ekstrand-Hammarström B, Popp M et al. (2011) The antibacterial activity of
Ga3+ is influenced by ligand complexation as well as the bacterial carbon source. Antimicrob
Agents Chemother 55 (12):5568–5580
Sader HS, Rhomberg PR, Flamm RK et al. (2017) WCK 5222 (cefepime/zidebactam) antimicrobial
activity tested against Gram-negative organisms producing clinically relevant ß-lactamases. J
Antimicrob Chemother 72(6):1696–1703
3 Single Molecule Non-cleavable Multiply Active Antibacterials
Naruto S, Mizuta H, Nishimura H (1976) A novel amination of isoquinolinium salts via nucleophilic
substitution reaction. Tetrahedron Lett 17 (19):1597–1600
Nasr T, Bondock S, Ibrahim TM et al. (2020) New acrylamide-sulfisoxazole conjugates as
dihydropteroate synthase inhibitors. Bioorg Med Chem 28 (9):115444
Nechepurenko IV, Salakhutdinov NF, Tolstikov GA (2010) Berberine chemistry and biological
activity. Chem Sustain Dev 18:1–23
Okano A, Isley N, Boger D (2017) Peripheral modifications of [[CH 2 NH]Tpg 4] vancomycin
with added synergistic mechanisms of action provide durable and potent antibiotics. Proc Natl
Acad Sci U.S.A. 114:201704125
Oldfield E, Feng X (2014) Resistance-resistant antibiotics. Trends Pharmacol Sci 35 (12):664–674
Olleik H, Yacoub T, Hoffer L et al. (2020) Synthesis and evaluation of the antibacterial activities
of 13-substituted berberine derivatives. Antibiotics 9 (7):381
Opperman TJ, Nguyen ST (2015) Recent advances toward a molecular mechanism of efflux pump
inhibition. Front Microbiol 6: Article 421
Owens B (2017) Solithromycin rejection chills antibiotic sector. Nat Biotechnol 35 (3):187–188
Ozçelik B, Kartal M, Orhan I (2011) Cytotoxicity, antiviral and antimicrobial activities of alkaloids,
flavonoids, and phenolic acids. Pharm Biol 49 (4):396–402
Park KD, Lee JH, Kim SH et al. (2006) Synthesis of 13-(substituted benzyl) berberine and
berberrubine derivatives as antifungal agents. Bioorg Med Chem Lett 16 (15):3913–3916
Parker EN, Drown BS, Geddes EJ et al. (2020) Implementation of permeation rules leads to a FabI
inhibitor with activity against Gram-negative pathogens. Nat Microbiol 5 (1):67–75
Parkes AL, Yule IA (2016) Hybrid antibiotics - clinical progress and novel designs. Expert Opin
Drug Discov 11 (7):665–680
Parmar A, Iyer A, Lloyd DG et al. (2017) Syntheses of potent teixobactin analogues against
methicillin-resistant Staphylococcus aureus (MRSA) through the replacement of l-alloenduracididine with its isosteres. Chem Commun 53 (55):7788–7791
Peek J, Lilic M, Montiel D et al. (2018) Rifamycin congeners kanglemycins are active against
rifampicin-resistant bacteria via a distinct mechanism. Nat Commun 9 (1):4147
Peek J, Xu J, Wang H et al. (2020) A semisynthetic Kanglemycin shows in vivo efficacy against
high-burden rifampicin resistant pathogens. ACS Infect Dis 6:2431–2440
Peterson RM, Huang T, Rudolf JD et al. (2014) Mechanisms of self-resistance in the platensimycinand platencin-producing Streptomyces platensis MA7327 and MA7339 strains. Chem Biol 21
(3):389–397
Pitts CR, Bornemann D, Liebing P et al. (2019) Making the SF 5 group more accessible: A gasreagent-free approach to aryl tetrafluoro-λ 6 -sulfanyl chlorides. Angew Chem Int Ed 58:1950–
1954
Pokrovskaya V, Baasov T (2010) Dual-acting hybrid antibiotics: a promising strategy to combat
bacterial resistance. Expert Opin Drug Discov 5 (9):883–902
Rajendran L, Knölker HJ, Simons K (2010) Subcellular targeting strategies for drug design and
delivery. Nat Rev Drug Discov 9 (1):29–42
Ramesh R, Reddy DS (2018) Quest for novel chemical entities through incorporation of silicon in
drug scaffolds. J Med Chem 61 (9):3779–3798
Richter MF, Drown BS, Riley AP et al. (2017) Predictive compound accumulation rules yield a
broad-spectrum antibiotic. Nature 545 (7654):299–304
Roselli M, Cavalluzzi MM, Bruno C et al. (2016) Synthesis and evaluation of berberine derivatives
and analogs as potential antiacetylcholinesterase and antioxidant agents. Phytochem Lett 18:150–
156
Rzhepishevska O, Ekstrand-Hammarström B, Popp M et al. (2011) The antibacterial activity of
Ga3+ is influenced by ligand complexation as well as the bacterial carbon source. Antimicrob
Agents Chemother 55 (12):5568–5580
Sader HS, Rhomberg PR, Flamm RK et al. (2017) WCK 5222 (cefepime/zidebactam) antimicrobial
activity tested against Gram-negative organisms producing clinically relevant ß-lactamases. J
Antimicrob Chemother 72(6):1696–1703