Dihydrofolate Reductase Inhibitors, Nitroheterocycles (Furans), and 8-Hydroxyquinolines

Veyssier, P; Bryskier, A.

doi:10.1128/9781555815929.ch35

Cited by 10 publications

(6 citation statements)

References 10 publications

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“…Flammazine cream contains 1% of silver sulfadiazine as a main ingredient and this has broad antimicrobial activity against gram- negative and gram-positive bacteria as well as yeasts. The general mechanism of activity of sulfonamides is based on the inhibition of the bacterial enzyme dihydropteroate synthetase involved in the folate pathway [ 27 ]. Silver ions, in turn, are capable to inhibit microbial growth due to several mechanisms such as protein and enzyme inactivation and the blocking of replication and transcription processes by intercalating into DNA molecules [ 28 , 29 ].…”

Section: Resultsmentioning

confidence: 99%

“…The exact mechanism of mafenide acetate’s activity is also unknown, except that it differs from that of other sulfonamides [ 27 ]. Mafenide is particularly effective for the treatment of burn wounds because it is agent that most effectively penetrates the eschar, and is therefore capable of suppressing dense bacterial proliferation beneath the eschar surface.…”

Section: Resultsmentioning

confidence: 99%

“…Nitrofural is the active ingredient of Furacin ointment and, next to being bactericidal it also expresses anti-trypanosomal, anti-fungal activity and it is widely used in human and animal medicine. Nitrofural inhibits several bacterial enzymes, especially those involved in the aerobic and anaerobic degradation of glucose and pyruvate although the exact mechanism of action is unknown [ 27 , 31 ]. Phage activity was not much affected by incubation in Furacin, and only the A .…”

Section: Resultsmentioning

confidence: 99%

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Stability of bacteriophages in burn wound care products

et al. 2017

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Bacteriophages could be used along with burn wound care products to enhance antimicrobial pressure during treatment. However, some of the components of the topical antimicrobials that are traditionally used for the prevention and treatment of burn wound infection might affect the activity of phages. Therefore, it is imperative to determine the counteraction of therapeutic phage preparations by burn wound care products before application in patients. Five phages, representatives of two morphological families (Myoviridae and Podoviridae) and active against 3 common bacterial burn wound pathogens (Acinetobacter baumannii, Pseudomonas aeruginosa and Staphylococcus aureus) were tested against 13 different products commonly used in the treatment of burn wounds. The inactivation of the phages was quite variable for different phages and different products. Majority of the anti-infective products affected phage activity negatively either immediately or in the course of time, although impact was not always significant. Products with high acidity had the most adverse effect on phages. Our findings demonstrate that during combined treatment the choice of phages and wound care products must be carefully defined in advance.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Stability of bacteriophages in burn wound care products

et al. 2017

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“…These drugs act through suppressing dihydropteroate synthase DHPS enzyme. [42,43] In the light of medicinal attributes of pyrazole and pyrimidine heterocycles and our work related to the discovery of bioactive candidates, [44 -56] we introduce herein the design, construction and antimicrobial screening of novel pyrazole-pyrimidine hybrids utilizing fragment-based drug design approach. Our scope in this study was to construct novel pyrazole-pyrimidine derivatives via the merge between pyrimidine core and pyrazole nucleus which are important scaffolds as antimicrobial agents with dihydropteroate synthase inhibitory effect.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Docking Study of Pyrazolohydrazinopyrimidin‐4‐one Derivatives and Their Application as Antimicrobials

Bakr

Alolyyan

Elkanzi

et al. 2023

Chemistry & Biodiversity

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New series of pyrazoles 4a-c and pyrazolopyrimidines 5a -f had been constructed. The newly synthesized compounds were assessed for their antimicrobial activity towards E. coli and P. aeruginosa (gram -ve bacteria), B. subtilis and S. aureus (gram + ve bacteria) and A. flavus and C. albicans (representative of fungi). The pyrazolylpyrimidine-2,4-dione derivative 5b is the most active candidate against B. subtilis (MIC = 60 μg/mL) and P. aeruginosa (MIC = 45 μg/mL). Regarding antifungal potential, compound 5f was the most effective against A. flavus (MIC = 33 μg/mL). Similarly, compound 5c displayed strong antifungal activity towards C. Albicans (MIC = 36 μg/mL) in reference to amphotericin B (MIC = 60 μg/mL). Finally, the novel compounds had been docked inside dihydropteroate synthase (DHPS) to suggest the binding mode of these compounds.

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“…6 The 3,4,5trimethoxybenzyl analogue in this series, trimethoprim (TMP), is the most widely used DHFR antibacterial drug and has been used successfully for 5 decades to treat a variety of bacterial diseases. 7 Trimethoprim is often used in combination with sulfmethoxazole (brand name Bactrim) because of the high degree of synergy between sulfa drugs, which act on the enzyme dihydropteroate synthase, and DHFR-based antibacterial agents. Currently, one of the uses for sulfmethoxazole is to treat CA-MRSA infections where an oral agent with anti-MRSA activity is needed.…”

Section: ■ Introductionmentioning

confidence: 99%

Structure-Based Design of New Dihydrofolate Reductase Antibacterial Agents: 7-(Benzimidazol-1-yl)-2,4-diaminoquinazolines

et al. 2014

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A new series of dihydrofolate reductase (DHFR) inhibitors, the 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines, were designed and optimized for antibacterial potency and enzyme selectivity. The most potent inhibitors in this series contained a five-membered heterocycle at the 2-position of the benzimidazole, leading to highly potent and selective compounds that exploit the differences in the size of a binding pocket adjacent to the NADPH cofactor between the bacterial and human DHFR enzymes. Typical of these compounds is 7-((2-thiazol-2-yl)benzimidazol-1-yl)-2,4 diaminoquinazoline, which is a potent inhibitor of S. aureus DHFR (Ki = 0.002 nM) with 46700-fold selectivity over human DHFR. This compound also has high antibacterial potency on Gram-positive bacteria with an MIC versus wild type S. aureus of 0.0125 μg/mL and a MIC versus trimethoprim-resistant S. aureus of 0.25 μg/mL. In vivo efficacy versus a S. aureus septicemia was demonstrated, highlighting the potential of this new series.

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Dihydrofolate Reductase Inhibitors, Nitroheterocycles (Furans), and 8-Hydroxyquinolines

Cited by 10 publications

References 10 publications

Stability of bacteriophages in burn wound care products

Stability of bacteriophages in burn wound care products

Design, Synthesis, Docking Study of Pyrazolohydrazinopyrimidin‐4‐one Derivatives and Their Application as Antimicrobials

Structure-Based Design of New Dihydrofolate Reductase Antibacterial Agents: 7-(Benzimidazol-1-yl)-2,4-diaminoquinazolines

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