- Synthesis of arylfuran derivatives as potential antibacterial agents
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Bacterial infections represent a serious health care problem mainly due to the misuse and overuse of antibiotics, with consequent emergence of multidrug resistant bacterial strains. Then, because the urgent need to find novel and alternative antibacterial agents, the present work focuses on the synthesis of arylfuran derivatives with potential antimicrobial activity. Eighteen arylfuran derivatives were synthesized and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Among them, seven compounds containing an amino group in their structure showed activity, with compound 24 being the most effective against both Gram-negative (E. coli, MIC = 49 μM) and Gram-positive (S. aureus, MIC = 98 μM) bacteria, besides having exhibited a modest activity against P. aeruginosa (MIC = 770 μM). In addition, based on in silico studies, this is a druglike compound since it does not violate any rules for predicting oral bioavailability. In this context, the significant antibacterial potential and the low similarity with known antibiotics indicate the innovative aspect of compound 24.
- Andrade, Marina M. S.,Protti, ícaro F.,Maltarollo, Vinícius G.,da Costa, Ygor F. G.,de Moraes, Wesley G.,Moreira, Nicole F.,Garcia, Giovana G.,Caran, Gabriel F.,Ottoni, Flaviano M.,Alves, Ricardo J.,Moreira, Carolina P. S.,Martins, Helen R.,Alves, Maria Silvana,de Oliveira, Renata B.
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p. 1074 - 1086
(2021/02/26)
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- A phenyl [...] hERG potassium ion channel of small molecule fluorescent probe and its application (by machine translation)
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The invention discloses a phenyl furan small molecule fluorescent probe and its application. The general structure of the fluorescent probe shown in formula (I): In the formula, R 1 is halogen, a mono-substituted alkyl or alkoxy substituent base or many ; R 2 to fluorophore; n=1-6 ; ethylene in between with the fluorophore containing 1-6 is connected with the carbon of the alkyl chain. The fluorescence probe molecule can be used to mark hERG potassium ion channel, can be used for hERG the activity of the potassium ion channel inhibitors screening and listing pharmaceutical evaluation of the cardiac toxicity, in addition can also as a tool to medicine hERG potassium ion channel related phannacological, pathology and physiol research. Furthermore, this kind of compound preparation method mild reaction conditions, the raw material is cheap and easy to obtain, operation and after treatment is simple. (by machine translation)
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