Bactericidal and Morphological Effects of NE-2001, a Novel Synthetic Agent Directed against
            <i>Helicobacter pylori</i>

Dai, Guofei; Cheng, Ni; Dong, Lei; Muramatsu, Mutsumi; Xiao, Shu–Dong; Wang, Mingwei; Zhu, Dunru

doi:10.1128/aac.49.8.3468-3473.2005

Cited by 14 publications

(17 citation statements)

References 22 publications

(14 reference statements)

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“…The core structure of both series A and B compounds were designed based on NE-2001, whose putative target may involve a proteinase of microbial origin [22] . OpdA (EC 3.4.24.70) is the major soluble enzyme in Escherichia coli capable of hydrolyzing the free lipoprotein signal peptide in vitro [45] .…”

Section: Discussionmentioning

confidence: 99%

“…A class of guanidine-containing antibacterial agents that targets a proteinase of microbial origin was identified as competitive trypsin inhibitors in vitro and consists of various aromatic esters of trans-4-guanidinomethylcyclohexanecarboxylic acid (GMCHA) [17][18][19][20] . For instance, trans-4guanidinomethyl cyclohexane carboxylic acid (4-[4-{4-methylbenzyloxy carbonyl}phenyl] phenylester) (TG44), a derivative of GMCHA [21] , and 4-guanidinomethyl benzoic acid (4-[4-{4-methylben zyloxy carbon yl}phenyl] phenylester) (NE-2001; Figure 1) are both selective synthetic antibiotic agents directed against Helicobacter pylori (H pylori ) [22] . TG44, which is undergoing clinical development, possesses rapid bactericidal activity and is useful for eradicating not only the antibiotic-susceptible, but also the antibiotic-resistant strains of H pylori by monotherapy [21] .…”

Section: Introductionmentioning

confidence: 99%

“…TG44, which is undergoing clinical development, possesses rapid bactericidal activity and is useful for eradicating not only the antibiotic-susceptible, but also the antibiotic-resistant strains of H pylori by monotherapy [21] . As a drug candidate, NE-2001 displays superior anti-H pylori efficacy on clinical isolates either resistant to metronidazole or resistant to both metronidazole and clarithromycin [22] .…”

Section: Introductionmentioning

confidence: 99%

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Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Yang

Xie³

et al. 2008

Acta Pharmacologica Sinica

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Aim: The aim of the present study was to design, synthesize, and evaluate novel antibacterial agents, derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide. Methods: A total of 44 derivatives of aryl-4-guanidinomethylbenzoate (series A) and N-aryl-4-guanidinomethylbenzamide (series B) were synthesized and their antibacterial activities were assessed in vitro against a variety of Gram-positive and Gram-negative bacteria by an agar dilution method. Results: Twelve compounds showed potent bactericidal effects against a panel of Gram-positive germs, including methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), vancomycin-intermediate Staphylococcus aureus (VISA), and methicillin-resistant coagulase-negative staphylococci (MRCNS), with minimum inhibitory concentrations (MIC) ranging between 0.5 and 8 µg/mL, which were comparable to the MIC values of several marketed antibiotics. They exhibited weak or no activity on the Gram-negative bacteria tested. In addition, these compounds displayed high inhibitory activities towards oligopeptidase B of bacterial origin. Conclusion: In comparison with the previously reported MIC values of several known antibiotics, the derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide showed comparable in vitro bactericidal activities against VRE and VISA as linezolid. Their growth inhibitory effects on MRSA were similar to vancomycin, but were less potent than linezolid and vancomycin against MRCNS. This class of compounds may have the potential to be developed into narrow spectrum antibacterial agents against certain drug-resistant strains of bacteria.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Yang

Xie³

et al. 2008

Acta Pharmacologica Sinica

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“…The ministry of health should have an effective drug control policy. Furthermore, there is the need to continue the evaluation of new treatment agents such as NE-2001 [20], older agents such as nitrofurantoin [21] or introduction of herbal management in order to eradicate Helicobacter pylori. Future case-control studies employing larger sample size are needed to demonstrate the effectiveness or otherwise of therapy in the different patient groups.…”

Section: Resultsmentioning

confidence: 99%

Determination of Antibiotic Sensitivity Pattern of <i>Helicobacter pylori</i> Isolates from South India Population

Ahmed¹,

Ghebremedhin²,

Khan³

et al. 2012

AiM

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Introduction:The importance of H. pylori as an etiological agent in gastroduodenal disease had suggested antibiotic treatment as a main target for the elimination of infection. The successful eradication of H. pylori infection was shown to resolve the gastritis, dramatically accelerate ulcer healing, reduce ulcer recurrence and the prophylactic effect on the recurrence of ulcer bleeding. Materials and Methods: In the present study a total six antimicrobial agents such as Ciprofloxacin, Metronidazole, Norfloxacin, Tetracyclin, Amoxycillin and Clarithromycin were used against 100 clinical isolates from patients with peptic ulcer, and non-ulcer dyspepsia. H. pylori was isolated from the gastric biopsies obtained from the clinical subjects. Results: Results of our study showed 100% resistance to Metronidazole (MIC > 256 μg/ml). 97% of the isolates were observed sensitive to Ciprofloxacin (MIC 0.38 μg), whereas Tetracyclin showed 96% sensitivity (MIC 0.25 μg -0.125 μg). Resistance to amoxycillin, Norfloxacin, and Clarithromycin were 80%, 38% and 76% respectively (MIC > 256 μg/ml). Conclusion: It is observed that 96% -97% of the clinical isolates were sensitive to Tetracycline and ciprofloxacin, where all isolates were found to be resistant to Metronidazole. Resistance to Amoxycillin and Clarithromycin were 80% and 76% respectively. Studies attributed the high level of resistance to the frequent use of the drugs to treat various other infections and ineffective drug control policy.

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“…The time–kill study was performed according to CLSI guidelines (NCCLS, ). Helicobacter pylori ATCC 43579 was cultured in 10 mL of Mueller–Hinton broth supplemented with 10% fetal bovine serum (FBS) and incubated at 37 °C with 10% CO 2 for 24 h (Dai et al , ). A final inoculum was measured at time 0; subsequent viable counts were carried out at 3, 5, 7 and 24 h. The killing rates were determined by plotting log10 colony counts (CFU/mL) against time.…”

Section: Methodsmentioning

confidence: 99%

Combination Studies of Eucalyptus torelliana F. Muell. Leaf Extracts and Clarithromycin on Helicobacter pylori

Lawal

Adeniyi

Moody

et al. 2012

Phytotherapy Research

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Helicobacter pylori is a Gram-negative bacillus that is associated with the development of gastritis and peptic ulcer disease (PUD). In Nigeria, leaf extracts of Eucalyptus torelliana F. Muell. are used in traditional medicine to treat PUD and other gastrointestinal ailments. The additive and synergistic effects of E. torelliana leaf extracts, in combination with clarithromycin, were investigated using two types of H. pylori strains (ATCC 43629, ATCC 43579) and four clinical isolates of H. pylori (Ed, A2, G1-1, 5514) in the checkerboard assay and the fractional inhibitory concentration (FIC) index. A time-kill study was also performed on the strain ATCC 43579. The results showed that the E. torelliana extract inhibited the growth of all H. pylori strains, and the addition of one of the isolated active compounds, namely compound 2 (a substituted pyrenyl ester) enhanced the activity of clarithromycin. The minimum inhibitory concentration values of clarithromycin and the botanical compound were reduced twofold (from 0.125 to 0.0625 µg/mL and > 100 to 50 µg/mL respectively). A 100% reduction in CFU/mL of H. pylori ATCC 43579 was observed with the combination of 0.25 µg/mL clarithromycin and 100 µg/mL and 200 µg/mL compound 2 after 3 h of exposure. The results of the investigation showed that the combination of botanical compounds and antibiotics may be beneficial in the treatment of H. pylori infections.

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Bactericidal and Morphological Effects of NE-2001, a Novel Synthetic Agent Directed against Helicobacter pylori

Cited by 14 publications

References 22 publications

Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Determination of Antibiotic Sensitivity Pattern of <i>Helicobacter pylori</i> Isolates from South India Population

Combination Studies of Eucalyptus torelliana F. Muell. Leaf Extracts and Clarithromycin on Helicobacter pylori

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Bactericidal and Morphological Effects of NE-2001, a Novel Synthetic Agent Directed against Helicobacter pylori

Cited by 14 publications

References 22 publications

Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Derivatives of aryl-4-guanidinomethylbenzoate and N-aryl-4-guanidinomethylbenzamide as new antibacterial agents: synthesis and bioactivity

Determination of Antibiotic Sensitivity Pattern of &lt;i&gt;Helicobacter pylori&lt;/i&gt; Isolates from South India Population

Combination Studies of Eucalyptus torelliana F. Muell. Leaf Extracts and Clarithromycin on Helicobacter pylori

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Determination of Antibiotic Sensitivity Pattern of <i>Helicobacter pylori</i> Isolates from South India Population