Pyrimidinetrione‐imidazoles as a Unique Structural Type of Potential Agents towards <i>Candida Albicans</i>: Design, Synthesis and Biological Evaluation

Sui, Yan-Fei; Ansari, Mohammad Fawad; Zhou, Cheng‐He

doi:10.1002/asia.202100146

Cited by 35 publications

(11 citation statements)

References 62 publications

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“…The release of cell constituents into the supernatant was measured according to the described method with little modifications . Cells (MRSA and P.…”

Section: Methodsmentioning

confidence: 94%

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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“…The release of cell constituents into the supernatant was measured according to the described method with little modifications . Cells (MRSA and P.…”

Section: Methodsmentioning

confidence: 94%

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

et al. 2022

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“…There have been three mechanisms of resistance against quinolones, including mutations of topoisomerases, decreased membrane permeability, and active drug efflux. − Hence, it is urgent to develop new candidates with low drug resistance trends. This study used reference drug norfloxacin as a positive control to test the drug resistance of S. A.…”

Section: Results and Discussionmentioning

confidence: 99%

New Efforts toward Aminothiazolylquinolones with Multitargeting Antibacterial Potential

Zhang

Battini

et al. 2023

J. Agric. Food Chem.

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New antibacterial 3-(aminothiazolyl)quinolones (ATQs) were designed and efficiently synthesized to counteract the growing multidrug resistance in animal husbandry. Bioactive assays manifested that N,N-dicyclohexylaminocarbonyl ATQ 10e and methyl ATQ 17a, respectively, showed better antibacterial behavior against Staphylococcus aureus ATCC 29213 and Pseudomonas aeruginosa than reference drug norfloxacin. Notably, highly active ATQ 17a with low hemolysis, negligible mammalian cytotoxicity, and good pharmacokinetic properties displayed low trends to induce resistance and synergistic combinations with norfloxacin. Preliminary mechanism exploration implied that representative ATQ 17a could inhibit the formation of biofilms and destroy bacterial membrane integrity, further binding to intracellular DNA and DNA gyrase to hinder bacterial DNA replication. ATQ 17a could also induce the production of excess reactive oxygen species and reduce bacterial metabolism to accelerate bacterial death. These results provided a promise for 3-(aminothiazolyl)quinolones as new potential multitargeting antibacterial agents to treat bacterial infection of animals.

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“…[ 14 ] A lot of investigations have found that bacterial cell membrane is a hopeful target in discovery of antibacterial drugs. [ 15 ] Therefore, the ability of pyrimidinone benzimidazole 9e to damage bacterial membrane was investigated.…”

Section: Resultsmentioning

confidence: 99%

A New Discovery towards Novel Skeleton of Benzimidazole‐Conjugated Pyrimidinones as Unique Effective Antibacterial Agents

et al. 2022

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Comprehensive Summary A class of new potential antibacterial agents with distinctive pyrimidinone benzimidazole skeleton was developed through nucleophilic substitution and Biginelli reaction starting from urea, ethyl 4‐chloroacetoacetate and various aldehydes. Some target molecules exhibited strong antibacterial activities, especially pyrimidinone benzimidazole hybrid 9e possessed the strongest inhibitory effects on the growth of E. faecalis and P. aeruginosa with a lower MIC value of 1 μg/mL than norfloxacin. Moreover, compound 9e displayed strong antibiofilm capacity, low drug resistance and excellent biosafety toward human red blood cells. Further research revealed that compound 9e could disrupt membrane integrity and cause leakage of cellular components such as proteins and nucleic acids. Meanwhile, compound 9e could decrease lactate dehydrogenase activity, block cell metabolism and interact with DNA in an intercalation manner. ADMET analysis predicated that molecule 9e possessed promising pharmacokinetic properties and good bioavailability profile.

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Pyrimidinetrione‐imidazoles as a Unique Structural Type of Potential Agents towards Candida Albicans: Design, Synthesis and Biological Evaluation

Cited by 35 publications

References 62 publications

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

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

New Efforts toward Aminothiazolylquinolones with Multitargeting Antibacterial Potential

A New Discovery towards Novel Skeleton of Benzimidazole‐Conjugated Pyrimidinones as Unique Effective Antibacterial Agents

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