Covalently linked kanamycin – Ciprofloxacin hybrid antibiotics as a tool to fight bacterial resistance

Shavit, Michal; Pokrovskaya, Varvara; Belakhov, V. V.; Baasov, Timor

doi:10.1016/j.bmc.2017.02.068

Cited by 48 publications

(22 citation statements)

References 31 publications

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“…The synthesis of the Cipro-NeoB/Cipro-KanA, which was active against a wide range of strains, is one of the most successful examples of this approach ( Figure 16 ). The MIC values of these hybrids were the same against resistant and non-resistant strains (AAC(6′), APH(3′), and AAC(6′)/APH(2″) [ 110 , 111 ]. This kind of aminoglycoside derivative, based on a hybrid structure, provides a promising drug with an unusual dual mechanism of action, a potent profile against AMEs, and reduced potential for generating bacterial resistance.…”

Section: Combination Therapymentioning

confidence: 99%

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

et al. 2018

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Resistance to aminoglycoside antibiotics has had a profound impact on clinical practice. Despite their powerful bactericidal activity, aminoglycosides were one of the first groups of antibiotics to meet the challenge of resistance. The most prevalent source of clinically relevant resistance against these therapeutics is conferred by the enzymatic modification of the antibiotic. Therefore, a deeper knowledge of the aminoglycoside-modifying enzymes and their interactions with the antibiotics and solvent is of paramount importance in order to facilitate the design of more effective and potent inhibitors and/or novel semisynthetic aminoglycosides that are not susceptible to modifying enzymes.

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Section: Combination Therapymentioning

confidence: 99%

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

et al. 2018

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“…A set of 12 hybrids 3 (Fig. ) that covalently linked CPFX and kanamycin A antibiotics was determined for their activities against both Gram‐negative and Gram‐positive bacteria, including drug‐resistant strains . In spite of all hybrids were less potent than CPFX against all of the tested strains, they were substantially more active than kanamycin A against Gram‐negative bacteria, and could overcome most dominant resistance mechanisms to aminoglycosides.…”

Section: Antibacterial Activitymentioning

confidence: 99%

Quinolone–Triazole Hybrids and their Biological Activities

Fan

Zhou

2018

Journal of Heterocyclic Chem

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Hybridization, a strategy based on the covalent fusion of two or more existing pharmacophores to create a single molecule with multiple mechanisms of action, represents an encourage approach in the development of new drugs with potential therapeutic application in several pathologies. Triazoles and quinolones occupy an important position in medicinal chemistry attribute to their various biological activities, so hybridization of these two pharmacophores may provide more effective candidates that might be able to prevent the drug resistance. This review outlines the biological activities of triazole–quinolone hybrids, and discusses their structure–activity relationship.

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“…3. Synthesis of new dual action antibiotics by linking two different antibiotic molecules [85][86][87]122]. That makes it much more difficult for bacteria to develop resistance to these drugs.…”

Section: Resultsmentioning

confidence: 99%

Fighting bacterial resistance: approaches, challenges, and opportunities in the search for new antibiotics.Part 1. Antibiotics used in clinical practice: mechanisms of action and the development of bacterial resistance

Zhivich

2017

Microbiology Independent Research Journal (MIR Journal)

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Hundreds of thousands of people are dying every year in the world from infections caused by drug resistant bacteria. Antibiotic resistance is a rapidly increasing problem mostly as a result of the worldwide overuse and misuse of antibiotics for conditions that do not require them. The rapid spread of antibiotic resistance in bacteria makes it necessary to intensify the development of new antibiotics and new methods to combat drug resistant bacteria. The goal of this publication is to review the approaches to finding new antibiotics that are active against drug resistant bacteria. The first part of this review is focused on an analysis of the mechanisms of action of antibiotics that are used in clinical practice as well as the mechanisms of bacterial resistance. The molecular structure and modes of action of these antibiotics are reviewed with examples of detailed mechanisms of drugs interaction with the targets in bacteria. General and specific mechanisms of bacterial resistance to these antibiotics are described. Examples of new antibiotics development active against the drug resistant bacteria are presented.

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Covalently linked kanamycin – Ciprofloxacin hybrid antibiotics as a tool to fight bacterial resistance

Cited by 48 publications

References 31 publications

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

Overcoming Aminoglycoside Enzymatic Resistance: Design of Novel Antibiotics and Inhibitors

Quinolone–Triazole Hybrids and their Biological Activities

Fighting bacterial resistance: approaches, challenges, and opportunities in the search for new antibiotics.Part 1. Antibiotics used in clinical practice: mechanisms of action and the development of bacterial resistance

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