New antibiotics against gram-positives: present and future indications

Morata, Laura; Soriano, Álex

doi:10.1016/j.coph.2015.07.004

Cited by 21 publications

(13 citation statements)

References 60 publications

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“…96, 102, 106-109 The drug is marketed as tedizolid phosphate, a prodrug formulation of tedizolid that is phosphorylated at the 5-position hydroxymethyl group. 110-112 Structurally similar to linezolid, tedizolid possesses the core oxazolidinone ring (A-ring) as well as the fluoro-phenyl B-ring.…”

Section: Discussionmentioning

confidence: 99%

Recent advances in the rational design and optimization of antibacterial agents

et al. 2016

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This review discusses next-generation antibacterial agents developed using rational, or targeted, drug design strategies. The focus of this review is on small-molecule compounds that have been designed to bypass developing bacterial resistance, improve the antibacterial spectrum of activity, and/or to optimize other properties, including physicochemical and pharmacokinetic properties. Agents are discussed that affect known antibacterial targets, such as the bacterial ribosome, nucleic acid binding proteins, and proteins involved in cell-wall biosynthesis; as well as some affecting novel bacterial targets which do not have currently marketed agents. The discussion of the agents focuses on the rational design strategies employed and the synthetic medicinal chemistry and structure-based design techniques utilized by the scientists involved in the discoveries, including such methods as ligand- and structure-based strategies, structure-activity relationship (SAR) expansion strategies, and novel synthetic organic chemistry methods. As such, the discussion is limited to small-molecule therapeutics that have confirmed macromolecular targets and encompasses only a fraction of all antibacterial agents recently approved or in late-stage clinical trials. The antibacterial agents selected have been recently approved for use on the U.S. or European markets or have shown promising results in phase 2 or phase 3 U.S. clinical trials.

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Section: Discussionmentioning

confidence: 99%

Recent advances in the rational design and optimization of antibacterial agents

et al. 2016

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“…[3,4] Diseases caused by drug-resistantb acteria may transfer their resistance to drug-susceptible bacteria that ultimately may act as reservoir of resistance to pathogenic organisms. [6] In fact, only af ew novel antibiotics againstG ram-positive bacteria have become available in recentyears, [7] such as the new cephalosporins ceftobiprolea nd ceftaroline, active against methicillin-resistant Staphylococcus aureus (MRSA), and the oxazolidinone tedizolid, which is active against clinically relevant pathogens such as MRSA, methicillin-susceptible S. aureus (MSSA), and various Streptococcus species. Moreover,t he emergence of AMR coincides with ad eclinei nt he rate of developmento fn ew antimicrobiala gents.…”

Section: Introductionmentioning

confidence: 99%

“…Moreover,t he emergence of AMR coincides with ad eclinei nt he rate of developmento fn ew antimicrobiala gents. [6] In fact, only af ew novel antibiotics againstG ram-positive bacteria have become available in recentyears, [7] such as the new cephalosporins ceftobiprolea nd ceftaroline, active against methicillin-resistant Staphylococcus aureus (MRSA), and the oxazolidinone tedizolid, which is active against clinically relevant pathogens such as MRSA, methicillin-susceptible S. aureus (MSSA), and various Streptococcus species. [8,9] In contrast, treating Gram-negative bacterial infections is more challenging because of the rapid antimicrobial resistance they develop.…”

Section: Introductionmentioning

confidence: 99%

The Outcomes of Decorated Prolines in the Discovery of Antimicrobial Peptides from Temporin‐L

et al. 2019

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Previously, we identified a potent antimicrobial analogue of temporin L (TL), [Pro3]TL, in which glutamine at position 3 was substituted with proline. In this study, a series of analogues in which position 3 is substituted with non‐natural proline derivatives, was investigated for correlations between the conformational properties of the compounds and their antibacterial, cytotoxic, and hemolytic activities. Non‐natural proline analogues with substituents at position 4 of the pyrrolidine ring were considered. Structure–activity relationship (SAR) studies of these analogues were performed by means of antimicrobial and cytotoxicity assays along with circular dichroism (CD) and NMR spectroscopic analyses for selected compounds. The most promising peptides were additionally evaluated for their activity against some representative veterinary microbial strains to compare with those from human strains. We identified novel analogues with interesting properties that make them attractive lead compounds.

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“…Many important bioactive compounds are widely used in medical services and health care (Khan 2016; Larsen and Matchkov 2016; Morata et al 2015). Many of these compounds are either microbial metabolites or their semi-synthetic derivatives (Golinska et al 2015; Sessitsch et al 2013; Stepniewska and Kuzniar 2013).…”

Section: Introductionmentioning

confidence: 99%

Validation of reference genes for normalization of gene expression by qRT-PCR in a resveratrol-producing entophytic fungus (Alternaria sp. MG1)

Che

Shi

et al. 2016

AMB Expr

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Alternaria sp. MG1, an endophytic fungus isolated from Vitis vinifera, can independently produce resveratrol, indicating that this species contains the key genes for resveratrol biosynthesis. Identification of these key genes is essential to understand the resveratrol biosynthesis pathway in this strain, which is currently unknown in microorganisms. qRT-PCR is an efficient and widely used method to identify the key genes related to unknown pathways at the level of gene expression. Verification of stable reference genes in this strain is essential for qRT-PCR data normalization, although results have been reported for other Alternaria sp. strains. In this study, nine candidate reference genes including TUBA, EF1, EF2, UBC, UFD, RPS5, RPS24, ACTB and 18S were evaluated for expression stability in a diverse set of six samples representing different growth periods. We compared cell culture conditions and an optimized condition for resveratrol production. The comparison of the results was performed using four statistical softwares. A combination of TUBA and EF1 was found to be suitable for normalization of Alternaria sp. MG1 in different developmental stages, and 18S was found to be the least stable. The reference genes verified in this study will facilitate further research to explore gene expression and molecular mechanisms as well as the improvement of secondary metabolite yields in Alternaria sp. MG1. To our knowledge, this is the first validation of reference genes in Alternaria with the capability to produce resveratrol. Additionally, these results provide useful guidelines for the selection of reference genes in other Alternaria species.Electronic supplementary materialThe online version of this article (doi:10.1186/s13568-016-0283-z) contains supplementary material, which is available to authorized users.

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New antibiotics against gram-positives: present and future indications

Cited by 21 publications

References 60 publications

Recent advances in the rational design and optimization of antibacterial agents

Recent advances in the rational design and optimization of antibacterial agents

The Outcomes of Decorated Prolines in the Discovery of Antimicrobial Peptides from Temporin‐L

Validation of reference genes for normalization of gene expression by qRT-PCR in a resveratrol-producing entophytic fungus (Alternaria sp. MG1)

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