Efficacy of two novel 2,2&amp;rsquo;-bifurans to inhibit methicillin-resistant Staphylococcus aureus infection in male mice in comparison to vancomycin

El‐Sayed, Wael M.; Hussin, Warda A; Ismail, Mohamed A.

doi:10.2147/dddt.s36437

Cited by 10 publications

(8 citation statements)

References 27 publications

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“…The total antioxidant activity and reducing power of bichalcophenes showed that compounds 1B, 3B, and 5B are in the lead with antioxidant activity of ∼30%–50% (Figure 2) of that of ascorbic acid at the same concentration. In our previous study, compound 1B showed a noticeable antioxidant activity in vivo and elevated the hepatic activities of glutathione reductase and glutathione peroxidase and reduced the elevated hepatic malondialdehyde and serum interleukin-6 in mice infected with methicillin-resistant Staphylococcus aureus 7. A third mechanism could be the direct interaction with the mutagens/metabolites and preventing their damaging effects 22.…”

Section: Resultsmentioning

confidence: 92%

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

El‐Sayed¹,

Hussin²

2013

DDDT

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Evaluation of the potential antimutagenic activities of new compounds by Ames assay has been of great interest for the development of novel therapeutics for many diseases including cancer. Ten novel bichalcophenes with in vitro and in vivo broad spectrum activities against various microbial strains were investigated throughout the present study for their cytotoxic, antioxidant, and antimutagenic potential in a Salmonella reverse mutation assay system against sodium azide (NaN3) and benzo[a]pyrene (B[a]P). At nontoxic concentrations, all bichalcophenes alone or in combination with NaN3 (1 μg/plate) or B[a]P (20 μM) with S9 mix were not mutagenic. The bichalcophenes significantly reduced NaN3- and B[a]P-induced mutagenicity under pre-exposure and co-exposure conditions in a concentration-independent manner. However, the antimutagenic activity of bichalcophenes against B[a]P varied depending on the exposure regimen, being more effective under pre-exposure conditions. The antimutagenic activity was correlated with a high antioxidant activity that could promote the DNA repair system. Bichalcophenes are least likely to interfere with the microsomal bioactivation of B[a]P. Monocationic bichalcophenes were superior to the corresponding mononitriles as antimutagenic agents against both mutagens investigated, possibly due to the higher nucleophilic centers they have which could bind and protect the bacterial DNA. Three monocationic compounds were shown to have a strong anticancer activity against the 58 cell line. Based on the results of the present investigation, monocationic compounds (1, 4, and 5B) will be selected for further time consuming and costly chemoprevention studies in animal models.

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Section: Resultsmentioning

confidence: 92%

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

El‐Sayed¹,

Hussin²

2013

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“… 9 Bithiophenes and oligothiophenes and their derivatives are important synthetic precursors for biologically active materials. 10 – 13 Oligothiophene compound α-terthienyl (I) ( Figure 1 ) is considered an anti-infective, antiviral, and photosensitizing agent. 14 , 15 …”

Section: Introductionmentioning

confidence: 99%

Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues

Ismail¹,

Arafa²,

Youssef³

et al. 2014

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A series of 15 monocationic bithiophenes and isosteres were prepared and subjected to in vitro antiproliferative screening using the full National Cancer Institute (NCI)-60 cell line panel, representing nine types of cancer. Among the nine types of cancer involved in a five-dose screen, non-small cell lung and breast cancer cell lines were the most responsive to the antiproliferative effect of the tested compounds, especially cell lines A549/ATCC, NCI-H322M, and NCI-H460, whereas compounds 1a, 1c, 1d, and 7 exhibited potent activity, with GI50 values (drug concentration that causes 50% inhibition of cell growth) from less than 10 nM to 102 nM. In addition, compounds 1c and 1d gave GI50 values of 73 nM and 79 nM, respectively, against the MDA-MB-468 breast cancer cell line. Structure–activity relationship findings indicated that the mononitriles were far less active than their corresponding monoamidines and, within the amidines series, the bioisosteric replacement of a thiophene ring by a furan led to a reduction in antiproliferative activity. Also, molecular manipulations, involving substitution on the phenyl ring, or its replacement by a pyridyl, or alteration of the position of the amidine group, led to significant alteration in antiproliferative activity. On the other hand, DNA studies demonstrated that these monoamidine bichalcophenes have promising ability to cleave the genomic DNA. These monoamidines show a wide range of DNA affinities, as judged from their DNA cleavage effect, which are remarkably sensitive to all kinds of structural modifications. Finally, the novel bichalcophenes were tested for their antioxidant property by the ABTS (2,2′-azino- bis(3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt) assay, as well as lipid and nitric oxide scavenging techniques, and were found to exhibit good-to-potent antioxidant abilities.

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“…As it is unlikely that bacteria could develop resistance to these novel compounds, their possible clinical effectiveness is suggested. Two of these bichalcophenes (1A and 1B) have been tested in mice and found to be not toxic 29. Treatment of methicillin-resistant Staphylococcus aureus -infected mice with these bichalcophenes resulted in significant reductions in the viable bacterial count in blood, liver, kidney, and spleen.…”

Section: Discussionmentioning

confidence: 99%

Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship

Hussin¹,

Ismail²,

El‐Sayed³

2013

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Antibiotic resistance is a major health problem; therefore, new antibacterial agents will need to be continuously developed. A series of novel bichalcophenes has been tested and found to have antimicrobial activity against selected bacteria. Due to the promising antimicrobial effects of these 4-substituted phenyl bichalcophene derivatives, the study reported here was launched to examine the interaction between novel bichalcophenes and tetracycline. The minimum inhibitory concentration values for all bichalcophenes were between 8 and 64 μM. Many of the bichalcophenes had synergistic activity that increased the inhibitory effect of tetracycline against bacterial growth, as indicated by the fractional inhibitory concentration index. The post-antibiotic effects of the novel bichalcophenes were determined. Many bichalcophenes were able to elongate the period required for bacteria to recover and grow after a brief exposure to tetracycline. Escherichia coli did not develop resistance to many bichalcophenes over a period of 7 days. A structural activity relationship could be characterized, as monocationic derivatives were more active than the corresponding mononitriles. The presence of a pyridyl group and/or furan ring reduced the activity, while the presence of a phenyl or thiophene ring enhanced the antibacterial activity. Our results suggest that bichalcophenes could be useful to elevate the shelf life of many antibiotics.

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Efficacy of two novel 2,2’-bifurans to inhibit methicillin-resistant Staphylococcus aureus infection in male mice in comparison to vancomycin

Cited by 10 publications

References 27 publications

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues

Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship

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Efficacy of two novel 2,2&rsquo;-bifurans to inhibit methicillin-resistant Staphylococcus aureus infection in male mice in comparison to vancomycin

Cited by 10 publications

References 27 publications

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2&#39;-bichalcophenes and aza-analogs

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2&#39;-bichalcophenes and aza-analogs

Anticancer, antioxidant activities, and DNA affinity of novel monocationic bithiophenes and analogues

Novel 4-substituted phenyl-2,2&#39;-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship

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Efficacy of two novel 2,2’-bifurans to inhibit methicillin-resistant Staphylococcus aureus infection in male mice in comparison to vancomycin

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

Antimutagenic and antioxidant activity of novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs

Novel 4-substituted phenyl-2,2'-bichalcophenes and aza-analogs as antibacterial agents: a structural activity relationship