The Re-Discovering of Old Molecules to face the Antibiotic Crisis

Schillaci, Domenico

doi:10.4172/1948-5948.1000e121

Cited by 2 publications

(3 citation statements)

References 13 publications

(12 reference statements)

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“…It is estimated that at least two million people in the United States are infected each year, and 23,000 of them die because the underlying bacterial strains are not susceptible to treatment by any of the current antibiotics. 1,2 The World Health Organization, in a recent report on antimicrobial resistance in common bacterial pathogens, highlights that a postantibiotic era may start the 21st century. 3 Unfortunately, the current investments of drug companies in the development of new antibiotics are largely reduced in spite of the high medical need.…”

Section: Introductionmentioning

confidence: 99%

“…Drug-resistant bacteria are responsible for 5,000 deaths per year in the UK, and 25,000 deaths per year in Europe. It is estimated that at least two million people in the United States are infected each year, and 23,000 of them die because the underlying bacterial strains are not susceptible to treatment by any of the current antibiotics. , …”

Section: Introductionmentioning

confidence: 99%

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Sortase A Inhibitors: Recent Advances and Future Perspectives

et al. 2015

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Here, we describe the most promising small synthetic organic compounds that act as potent Sortase A inhibitors and cater the potential to be developed as antivirulence drugs. Sortase A is a polypeptide of 206 amino acids, which catalyzes two sequential reactions: (i) thioesterification and (ii) transpeptidation. Sortase A is involved in the process of bacterial adhesion by anchoring LPXTG-containing proteins to lipid II. Sortase A inhibitors do not affect bacterial growth, but they restrain the virulence of pathogenic bacterial strains, thereby preventing infections caused by Staphylococcus aureus or other Gram-positive bacteria. The efficacy of the most promising inhibitors needs to be comprehensively evaluated in in vivo models of infection, in order to select compounds eligible for the treatment of bacterial infections in humans.

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Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Sortase A Inhibitors: Recent Advances and Future Perspectives

et al. 2015

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“…Molecules 2015, 20, page-page 2 [12,13]. Valuable examples are provided by colistin, a polymixin produced by Paenibacillus polymyxa subspecies colistinus [14,15], or temocillin, fosfomycin, mecillinam, nitrofurantoin and chloramphenicol for multi drug resistant (MDR) Gram-negative bacteria, and trimethoprim-sulfamethoxazole for methicillin-resistant Staphylococcus aureus (MRSA) [16].…”

Section: Halogenated Pyrroles Related To Pyrrolomycinsmentioning

confidence: 99%

Pharmaceutical Potential of Synthetic and Natural Pyrrolomycins

et al. 2015

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Abstract:The emergence of antibiotic resistance is currently considered one of the most important global health problem. The continuous onset of multidrug-resistant Gram-positive and Gram-negative bacterial strains limits the clinical efficacy of most of the marketed antibiotics. Therefore, there is an urgent need for new antibiotics. Pyrrolomycins are a class of biologically active compounds that exhibit a broad spectrum of biological activities, including antibacterial, antifungal, anthelmintic, antiproliferative, insecticidal, and acaricidal activities. In this review we focus on the antibacterial activity and antibiofilm activity of pyrrolomycins against Gram-positive and Gram-negative pathogens. Their efficacy, combined in some cases with a low toxicity, confers to these molecules a great potential for the development of new antimicrobial agents to face the antibiotic crisis.

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The Re-Discovering of Old Molecules to face the Antibiotic Crisis

Cited by 2 publications

References 13 publications

Sortase A Inhibitors: Recent Advances and Future Perspectives

Sortase A Inhibitors: Recent Advances and Future Perspectives

Pharmaceutical Potential of Synthetic and Natural Pyrrolomycins

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