Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms

Sui, Yan-Fei; Ansari, Mohammad Fawad; Fang, Bo; Zhang, Shaolin; Zhou, Cheng‐He

doi:10.1016/j.ejmech.2021.113557

Cited by 43 publications

(17 citation statements)

References 79 publications

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“…To further gain a clear intercalative binding mode of DNA with compounds 4d or 18b , a well-known DNA intercalator acridine orange (AO) was used to conduct the competitive binding assay. − As presented in Figure A,B, the fluorescence intensity gradually decreased with the additions of compounds 4d or 18b , signifying that compound 4d or 18b has capacity to replace AO in DNA–AO complex to insert into DNA, exerting the powerful antibacterial activity.…”

Section: Results and Discussionmentioning

confidence: 99%

Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

et al. 2021

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Natural berberine-derived azolyl ethanols as new structural antibacterial agents were designed and synthesized for fighting with dreadful bacterial resistance. Partial target molecules exhibited potent activity against the tested strains, particularly, nitroimidazole derivative 4d and benzothiazole-2-thoil compound 18b, with low cytotoxicity both exerted strong antibacterial activities against multidrug-resistant Escherichia coli at low concentrations as 0.007 and 0.006 mM, respectively. Meanwhile, the active compounds 4d and 18b possessed the ability to rapidly kill bacteria and observably eradicate the E. coli biofilm by reducing exopolysaccharide content to prevent bacterial adhesion, which was conducive to alleviating the development of E. coli resistance. Preliminary mechanistic explorations suggested that the excellent antibacterial potential of molecules 4d and 18b might be attributed to their ability to disintegrate membrane, accelerate ROS accumulation, reduce bacterial metabolism, and intercalate into DNA groove. These results provided powerful information for the further exploitation of natural berberine derivatives against bacterial pathogens.

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Section: Results and Discussionmentioning

confidence: 99%

Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

et al. 2021

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“…DNA has been considered as a potent drug target and is widely utilized for the design and development of new efficient antibacterial drugs. − Therefore, the interaction mode of compound 7d and DNA was explored using AO spectral probe. The absorption spectra of DNA–AO complex varying with compound 7d concentrations are recorded in Figure S5A.…”

Section: Resultsmentioning

confidence: 99%

Natural Berberine-Hybridized Benzimidazoles as Novel Unique Bactericides against Staphylococcus aureus

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Ansari

Fang

et al. 2021

J. Agric. Food Chem.

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Natural berberine-hybridized benzimidazoles as potential antibacterial agents were constructed to treat Staphylococcus aureus infection in the livestock industry. Bioassay showed that some new berberine-benzimidazole hybrids exhibited potent antibacterial efficacies, especially, the 2,4-dichlorobenzyl derivative 7d not only showed strong activity against S. aureus ATCC 29213 with the MIC value of 0.006 mM but also effectively eradicated bacterial biofilm and exhibited low toxicity toward mammalian cells. The drug combination experiments showed that compound 7d together with norfloxacin could enhance the antibacterial efficacy. Moreover, the 2,4-dichlorobenzyl derivative 7d did not show obvious propensity to develop bacterial resistance. Preliminary mechanism studies revealed that the active molecule 7d could damage the membrane integrity, stimulate ROS generation, and bind with DNA as well as S. aureus sortase A, thus exerting powerful antibacterial ability. In light of these facts, berberine-benzimidazole hybrid 7d showed a large potentiality as a new bactericide for treating S. aureus in the livestock industry.

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“…Outer-membrane permeability assay using the N -phenylnapthylamine (NPN) probe was performed according to the reported procedures with little modifications . Stationary-phase bacteria (P.…”

Section: Methodsmentioning

confidence: 99%

“…Outer-membrane permeability assay using the N-phenylnapthylamine (NPN) probe was performed according to the reported procedures with little modifications. 62 Stationary-phase bacteria (P. aeruginosa ATCC 27853) were harvested, washed, and resuspended in 5 mM glucose and 5 mM HEPES buffer (1:1) at pH 7.2 to OD 600 nm around 0.5 bacterial solutions. Then, the tested compound 23b or 23c (1 μg/ mL) and NPN dye (10 μM, 50 μL) were added to the wells containing P. aeruginosa ATCC 27853 bacterial suspension, respectively.…”

Section: ■ Conclusionmentioning

confidence: 99%

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

et al. 2022

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Novel carbazole-oxadiazoles were developed as new potential antibacterial agents to combat dreadful resistance. Some target compounds displayed predominant inhibitory effects on the tested Gram-positive and -negative bacteria, and carbazole-oxadiazoles 5g, 5i–k, 16a–c, and tetrazole analogues 23b–c were found to be efficient in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853 (MICs = 0.25–4 μg/mL). Furthermore, compounds 5g and 23b–c not only possessed rapid bactericidal ability and low tendency to develop resistance but also exhibited low cytotoxic effects toward Hek 293T, HeLa, and red blood cells (RBCs), especially molecule 5g also showed low toxicity in vivo, which showed the therapeutic potential of these compounds. Further exploration indicated that compounds 5g, 5i, and 23b–c could disintegrate the integrity of bacterial cell membranes to leak the cytoplasmic contents, thus exerting excellent antibacterial effects. These facts mean that carbazole-based antibacterial agents might have bright prospects in confronting bacterial infections.

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Discovery of novel purinylthiazolylethanone derivatives as anti-Candida albicans agents through possible multifaceted mechanisms

Cited by 43 publications

References 79 publications

Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

Natural Berberine-Hybridized Benzimidazoles as Novel Unique Bactericides against Staphylococcus aureus

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

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