118
3 Single Molecule Non-cleavable Multiply Active Antibacterials
Tomkiewicz D, Casadei G, Larkins-Ford J et al. (2010) Berberine-INF55 (5-nitro-2-phenylindole)
hybrid antimicrobials: Effects of varying the relative orientation of the berberine and INF55
components. Antimicrob Agents Chemother 54:3219–3224
Tumey LN, Boschelli DH, Bhagirath N et al. (2014) Identification and optimization of indolo[2,3c]quinoline inhibitors of IRAK4. Bioorg Med Chem Lett 24 (9):2066–2072
Van Bambeke F, Pagès J-M, Lee V (2009) Inhibitors of bacterial efflux pumps as adjuvants in
antibacterial therapy and diagnostic tools for detection of resistance by efflux. In: Atta-ur-Rahman,
Choudhary MI (eds) Frontiers in anti-infective drug discovery, vol 1. Bentham Science, pp 138–
175
Van der Schyf CJ, Geldenhuys WJ (2009) Polycyclic compounds: ideal drug scaffolds for the design
of multiple mechanism drugs? Neurotherapeutics 6 (1):175–186
Van Miert S, Hostyn S, Maes BUW et al. (2005) Isoneocryptolepine, a synthetic indoloquinoline
alkaloid, as an antiplasmodial lead compound. J Nat Prod 68:674–677
Wang B, Deng A-J, Li Z-H et al. (2020) Syntheses and structure–activity relationships in growth inhibition activity against human cancer cell lines of 12 substituted berberine derivatives. Molecules
25 (8):1871
Wang J, Kodali S, Lee SH et al. (2007) Discovery of platencin, a dual FabF and FabH inhibitor with
in vivo antibiotic properties. Proc Natl Acad Sci 104 (18):7612–7616
Wang J, Tang J, Yu L-F et al. (2015) Berberine analogues: progress towards versatile applications.
Heterocycles 91:2233
Wang J, Yang T, Chen H et al. (2017a) The synthesis and antistaphylococcal activity of 9, 13disubstituted berberine derivatives. Eur J Med Chem 127:424–433
Wang K, Feng X, Chai L et al. (2017b) The metabolism of berberine and its contribution to the
pharmacological effects. Drug Metab Rev 49 (2):139–157
Wang YX, Pang WQ, Zeng QX et al. (2018) Synthesis and biological evaluation of new berberine
derivatives as cancer immunotherapy agents through targeting IDO1. Eur J Med Chem 143:1858–
1868
Whitty A, Zhong M, Viarengo L et al. (2016) Quantifying the chameleonic properties of macrocycles
and other high-molecular-weight drugs. Drug Disc Today 21(5):712–717
Wockhardt Discovery (2017) WCK 2349 (Oral prodrug). https://wockhardtdiscovery.com/wck2349-oral-prodrug/. Accessed 6 March 2017
Woods A, Rahman KM (2018) Antimicrobial molecules in the lung: formulation challenges and
future directions for innovation. Future Med Chem 10 (5):575–604
Xiao ZP, Wang XD, Wang PF et al. (2014) Design, synthesis, and evaluation of novel
fluoroquinolone-flavonoid hybrids as potent antibiotics against drug-resistant microorganisms.
Eur J Med Chem 80:92–100
Xue M, Yang Y, Chi X et al. (2015) Development of pseodorotaxanes and rotaxanes: From synthesis
to stimuli-responsive motions to applications. Chem Rev 115:7398–7501
Yang Y-S, Wei W, Hu X-X et al. (2019) Evolution and antibacterial evaluation of 8-hydroxycycloberberine derivatives as a novel family of antibacterial agents against MRSA. Molecules 24
(5):984
Yi S, Varun BV, Choi Y et al. (2018) A brief overview of two major strategies in diversity-oriented
synthesis: build/couple/pair and ring-distortion. Front Chem 6:507–507
Yin Z, Whittell LR, Wang Y et al. (2014) Discovery of lead compounds targeting the bacterial
sliding clamp using a fragment-based approach. J Med Chem 57(6):2799–2806
Yin Z, Whittell LR, Wang Y et al. (2015) Bacterial sliding clamp inhibitors that mimic the sequential
binding mechanism of endogenous linear motifs. J Med Chem 58 (11):4693–4702
Yuan Y, Pei J, Lai L (2020a) LigBuilder V3: a multi-target de novo drug design approach. Front
Chem 8:142
Yuan Y, Wang X, Xu X et al. (2020b) Evaluation of a dual-acting antibacterial agent, TNP-2092, on
gut microbiota and potential application in the treatment of gastrointestinal and liver disorders.
ACS Infect Dis 6 (5):820–831
3 Single Molecule Non-cleavable Multiply Active Antibacterials
Tomkiewicz D, Casadei G, Larkins-Ford J et al. (2010) Berberine-INF55 (5-nitro-2-phenylindole)
hybrid antimicrobials: Effects of varying the relative orientation of the berberine and INF55
components. Antimicrob Agents Chemother 54:3219–3224
Tumey LN, Boschelli DH, Bhagirath N et al. (2014) Identification and optimization of indolo[2,3c]quinoline inhibitors of IRAK4. Bioorg Med Chem Lett 24 (9):2066–2072
Van Bambeke F, Pagès J-M, Lee V (2009) Inhibitors of bacterial efflux pumps as adjuvants in
antibacterial therapy and diagnostic tools for detection of resistance by efflux. In: Atta-ur-Rahman,
Choudhary MI (eds) Frontiers in anti-infective drug discovery, vol 1. Bentham Science, pp 138–
175
Van der Schyf CJ, Geldenhuys WJ (2009) Polycyclic compounds: ideal drug scaffolds for the design
of multiple mechanism drugs? Neurotherapeutics 6 (1):175–186
Van Miert S, Hostyn S, Maes BUW et al. (2005) Isoneocryptolepine, a synthetic indoloquinoline
alkaloid, as an antiplasmodial lead compound. J Nat Prod 68:674–677
Wang B, Deng A-J, Li Z-H et al. (2020) Syntheses and structure–activity relationships in growth inhibition activity against human cancer cell lines of 12 substituted berberine derivatives. Molecules
25 (8):1871
Wang J, Kodali S, Lee SH et al. (2007) Discovery of platencin, a dual FabF and FabH inhibitor with
in vivo antibiotic properties. Proc Natl Acad Sci 104 (18):7612–7616
Wang J, Tang J, Yu L-F et al. (2015) Berberine analogues: progress towards versatile applications.
Heterocycles 91:2233
Wang J, Yang T, Chen H et al. (2017a) The synthesis and antistaphylococcal activity of 9, 13disubstituted berberine derivatives. Eur J Med Chem 127:424–433
Wang K, Feng X, Chai L et al. (2017b) The metabolism of berberine and its contribution to the
pharmacological effects. Drug Metab Rev 49 (2):139–157
Wang YX, Pang WQ, Zeng QX et al. (2018) Synthesis and biological evaluation of new berberine
derivatives as cancer immunotherapy agents through targeting IDO1. Eur J Med Chem 143:1858–
1868
Whitty A, Zhong M, Viarengo L et al. (2016) Quantifying the chameleonic properties of macrocycles
and other high-molecular-weight drugs. Drug Disc Today 21(5):712–717
Wockhardt Discovery (2017) WCK 2349 (Oral prodrug). https://wockhardtdiscovery.com/wck2349-oral-prodrug/. Accessed 6 March 2017
Woods A, Rahman KM (2018) Antimicrobial molecules in the lung: formulation challenges and
future directions for innovation. Future Med Chem 10 (5):575–604
Xiao ZP, Wang XD, Wang PF et al. (2014) Design, synthesis, and evaluation of novel
fluoroquinolone-flavonoid hybrids as potent antibiotics against drug-resistant microorganisms.
Eur J Med Chem 80:92–100
Xue M, Yang Y, Chi X et al. (2015) Development of pseodorotaxanes and rotaxanes: From synthesis
to stimuli-responsive motions to applications. Chem Rev 115:7398–7501
Yang Y-S, Wei W, Hu X-X et al. (2019) Evolution and antibacterial evaluation of 8-hydroxycycloberberine derivatives as a novel family of antibacterial agents against MRSA. Molecules 24
(5):984
Yi S, Varun BV, Choi Y et al. (2018) A brief overview of two major strategies in diversity-oriented
synthesis: build/couple/pair and ring-distortion. Front Chem 6:507–507
Yin Z, Whittell LR, Wang Y et al. (2014) Discovery of lead compounds targeting the bacterial
sliding clamp using a fragment-based approach. J Med Chem 57(6):2799–2806
Yin Z, Whittell LR, Wang Y et al. (2015) Bacterial sliding clamp inhibitors that mimic the sequential
binding mechanism of endogenous linear motifs. J Med Chem 58 (11):4693–4702
Yuan Y, Pei J, Lai L (2020a) LigBuilder V3: a multi-target de novo drug design approach. Front
Chem 8:142
Yuan Y, Wang X, Xu X et al. (2020b) Evaluation of a dual-acting antibacterial agent, TNP-2092, on
gut microbiota and potential application in the treatment of gastrointestinal and liver disorders.
ACS Infect Dis 6 (5):820–831