Potential Antimicrobial Isopropanol-Conjugated Carbazole Azoles as Dual Targeting Inhibitors of <i>Enterococcus faecalis</i>

Zhang, Yuan; Tangadanchu, Vijai Kumar Reddy; Cheng, Yu; Yang, Ren-Guo; Lin, Jian-Mei

doi:10.1021/acsmedchemlett.7b00514

Cited by 69 publications

(37 citation statements)

References 37 publications

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“…Antibacterial Activity . It is well documented from literature reports that natural alkaloid carbazole and its synthetic analogs have displayed notable antibacterial activity . Hence, we decided to evaluate these compounds against a panel of Gram‐positive ( S. aureus , B. subtilis ) and Gram‐negative ( E. coli , P. aeruginosa ) bacterial strains.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Carbazole Hybrids as Promising Antimicrobial Agents

Shaikh

Chandrasekaran

Palkar

et al. 2020

Chemistry & Biodiversity

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Two series of carbazole analogs of 8-methoxy-N-substituted-9H-carbazole-3-carboxamides (series 1) and carbazolyl substituted rhodanines (series 2) were synthesized through facile synthetic routes. All the final compounds from these two series were evaluated for their preliminary in vitro antifungal and antibacterial activity against four fungal (Candida albicans, Cryptococcus neoformans, Cryptococcus tropicalis and Aspergillus niger) and four bacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) strains, respectively. Among the tested compounds, three compounds of series 1 displayed promising antifungal and antibacterial activity, especially against C. neoformans and S. aureus. In addition, one compound of series 1 displayed notable antimicrobial activity (MIC: 6.25 μg/mL) against clinical isolates of C. albicans and C. neoformans (MIC: 12.5 μg/mL). From the second series, four compounds exhibited significant antifungal and antibacterial activity, especially against C. neoformans and S. aureus. The most active compound of series 2 displayed a prominent antimicrobial activity against C. neoformans (MIC: 3.125 μg/mL) and S. aureus (MIC: 1.56 μg/mL), respectively.

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Section: Resultsmentioning

confidence: 99%

Synthesis and Biological Evaluation of Novel Carbazole Hybrids as Promising Antimicrobial Agents

Shaikh

Chandrasekaran

Palkar

et al. 2020

Chemistry & Biodiversity

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“…In addition, the compounds also display appreciable toxicity in dark, which can be explained by the electrostatic interaction between the microbial cell membrane and the photosensitizers. 10 , 31 According to Zhang et al, 32 carbazole derivatives can permeate the membrane of E. coli cells and accumulate inside. We have performed an experiment by confocal scanning laser microscopy (CSLM) to study the viability membrane disruption of E. coli bacteria treated with BMEPC and BMEMC ( Figure S2 ).…”

Section: Resultsmentioning

confidence: 99%

Laser-Induced Antibacterial Activity of Novel Symmetric Carbazole-Based Ethynylpyridine Photosensitizers

Chen

Zheng

et al. 2018

ACS Omega

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In this study, two kinds of novel carbazole-based ethynylpyridine salts: 3,6-bis[2-(1-methylpyridinium)ethynyl]-9-pentyl-carbazole diiodide (BMEPC) and 3,6-bis[2-(1-methylpyridinium)ethynyl]-9-methyl-carbazole diiodide (BMEMC) have been employed as photosensitizers owing to their excellent antibacterial activity. These molecules possess symmetric A−π–D−π–A-type structures, which would bring in the unique optical properties. The inhibition zone measurement of a gradient concentration from 0 to 100 μM showed BMEPC and BMEMC photoinduced antibacterial activity against Escherichia coli. Diameters of zone of inhibition were up to 15 and 14 mm under laser irradiations. Under the exposure of the laser of 442 nm with a power density of 20 mW/cm2, the minimum inhibitory concentrations (MICs) of BMEPC on E. coli were between 3.5 and 6.9 μM and that of BMEMC were between 9.4 and 18.8 μM, respectively. In the dark experiments as a control, the MIC value is between 6.9 and 13.8 μM for BMEPC, whereas it is between 187.5 and 225.0 μM for BMEMC. By the comparison of the MIC values of BMEPC and BMEMC with laser irradiation and in dark, the laser-induced toxicity on bacteria is more evident, though both of the derivatives have dark toxicity. With the laser irradiation duration of 30 s and 10 min for BMEPC and BMEMC, respectively, the survival rate of E. coli approximates zero. An antibacterial mechanism has been proposed based on the electron paramagnetic resonance characterization, which indicates that a nitride radical is generated under laser irradiation. The carbazole-based ethynylpyridine photosensitizers would provide high potential for further applications in photodynamic therapy.

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“…9 ) were evaluated for their antibacterial activity against E. faecalis, S. aureus and E. coli by Zhang et al. [ 70 ]. Among them, compound 55a ( Fig.…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

214

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The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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Potential Antimicrobial Isopropanol-Conjugated Carbazole Azoles as Dual Targeting Inhibitors of Enterococcus faecalis

Cited by 69 publications

References 37 publications

Synthesis and Biological Evaluation of Novel Carbazole Hybrids as Promising Antimicrobial Agents

Synthesis and Biological Evaluation of Novel Carbazole Hybrids as Promising Antimicrobial Agents

Laser-Induced Antibacterial Activity of Novel Symmetric Carbazole-Based Ethynylpyridine Photosensitizers

An insight on medicinal attributes of 1,2,4-triazoles

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