Synthesis of N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamides and Their Inhibitory Activities against Secretory Phospholipase A2

Nakayama, Hitoshi; Ishihara, Keiichi; Akiba, Suminori; Uenishi, Jun’ichi

doi:10.1248/cpb.59.1069

Cited by 9 publications

(2 citation statements)

References 17 publications

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“…At present, the research on the toxicity of TfNH 2 is extremely limited. However, TfNH 2 is a specific inhibitor of phospholipases A2, which can regulate cell function, inflammatory response and antibacterial activity by affecting arachidonic acid and lysophospholipid pathways. , The high toxicity of TfNH 2 suggests that we should not only pay attention to the traditional long-chain PFAS, but also pay special heed to the potential health hazards and challenges brought by ultrashort-chain PFAS in the health prevention and control research of PFAS . Additionally, TFMS has the weakest toxic effect of all the detected PFAS, and only significantly affects the growth of nematodes, which may be related to its extremely short carbon chain (Figure B, Table S14).…”

Section: Resultsmentioning

confidence: 99%

Nontarget Analysis of Legacy and Emerging PFAS in a Lithium-Ion Power Battery Recycling Park and Their Possible Toxicity Measured Using High-Throughput Phenotype Screening

Qi,

Cao,

et al. 2024

Environ. Sci. Technol.

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Driven by the global popularity of electric vehicles and the shortage of critical raw materials for batteries, the spent lithium-ion power battery (LIPB) recycling industry has exhibited explosive growth in both quantity and scale. However, relatively little information is known about the environmental risks posed by LIPB recycling, in particular with regards to perfluoroalkyl and polyfluoroalkyl substances (PFAS). In this work, suspect screening and nontarget analysis were carried out to characterize PFAS in soil, dust, water and sediment from a LIPB recycling area. Twentyfive PFAS from nine classes were identified at confidence level 3 or above, including 13 legacy and 12 emerging PFAS, as well as two ultrashort-chain PFAS. Based on the target analysis of 16 PFAS, at least nine were detected in each environmental sample, indicating their widespread presence in a LIPB recycling area. Perfluorodecanoic acid, perfluorooctanesulfonic acid and trifluoromethanesulfonamide showed significant differences in the four phenotypic parameters (growth, movement, survival and fecundity) of Caenorhabditis elegans and were the most toxic substances in all target PFAS at an exposure concentration of 200 μM. Our project provides first-hand information on the existence and environmental risk of PFAS, facilitating the formulation of regulations and green development of the LIPB recycling industry.

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Section: Resultsmentioning

confidence: 99%

Nontarget Analysis of Legacy and Emerging PFAS in a Lithium-Ion Power Battery Recycling Park and Their Possible Toxicity Measured Using High-Throughput Phenotype Screening

Qi,

Cao,

et al. 2024

Environ. Sci. Technol.

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“…The compound 3g was found to possess antibacterial activity almost equivalent to standard drug. This is because it has been well established that the fluorine substituted molecules have got a significant important in modern medicinal chemistry[ 15 ] and it may be explained that the esters possess preferable lipophilicity and show optimal membrane permeability. The values for the antimicrobial studies of the compounds and the standard are represented in Table 1 .…”

Section: Resultsmentioning

confidence: 99%

Design and synthesis of quinazoline carboxylates against Gram-positive, Gram-negative, fungal pathogenic strains, and Mycobacterium tuberculosis

2014

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Aim:A novel series of ethyl 5-(4-substituted phenyl)-3-methyl-6,7,8,9-tetrahydro-5H-thiazolo[2,3-b] quinazoline-2-carboxylate 3a-3j, were synthesized, characterized by spectral, elemental analyses and screened for their in vitro antibacterial and Mycobacterium tuberculosis (MTB) activities.Materials and Methods:The in vitro antibacterial and antifungal activities were determined by agar well-diffusion and cup-plate agar diffusion methods and the anti-tuberculosis (TB) screening for test compounds were evaluated against MTB H37Rv strain by Resazurin assay.Results:Among the derivatives tested, most of the compounds were found to have potent activity against microbial strains. The structure-activity relationship point of view, introduced group that enhance the lipophilicity as well ester, substituted aromatic ring at thiazole quinazoline nucleus showed increasing antimicrobial and anti TB activity. The high level of activity shown by the compounds with electron withdrawing groups in the para position on the benzene ring (3 g) suggests that these compounds could serve as leads for development of novel synthetic compounds with enhanced antibacterial and anti TB activities.Conclusion:These results provide a further insight into the structural requirements for targeting thiazolo quinazoline carboxylate to develop potential new agents to combat TB treatment.

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Synthesis, characterization, and SAR studies of new (1H-indol-3-yl)alkyl-3-(1H-indol-3-yl)propanamide derivatives as possible antimicrobial and antitubercular agents

et al. 2013

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Synthesis of N-[2-(2,4-Difluorophenoxy)trifluoromethyl-3-pyridyl]sulfonamides and Their Inhibitory Activities against Secretory Phospholipase A2

Cited by 9 publications

References 17 publications

Nontarget Analysis of Legacy and Emerging PFAS in a Lithium-Ion Power Battery Recycling Park and Their Possible Toxicity Measured Using High-Throughput Phenotype Screening

Nontarget Analysis of Legacy and Emerging PFAS in a Lithium-Ion Power Battery Recycling Park and Their Possible Toxicity Measured Using High-Throughput Phenotype Screening

Design and synthesis of quinazoline carboxylates against Gram-positive, Gram-negative, fungal pathogenic strains, and Mycobacterium tuberculosis

Synthesis, characterization, and SAR studies of new (1H-indol-3-yl)alkyl-3-(1H-indol-3-yl)propanamide derivatives as possible antimicrobial and antitubercular agents

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