A very promising antibiofilm activity against Candida albicans from an in vitro screening for antimicrobial, antibiofilm and antiproliferative activity of new synthesized 4-cinnamamido- and 2-phenoxyacedamido-1H-pyrazol-5-yl)benzamides

被引:0
|
作者
Plescia, Fabiana [1 ]
Catania, Valentina [2 ]
D'Anneo, Antonella [3 ]
Raffa, Demetrio [1 ]
Lauricella, Marianna [4 ]
Schillaci, Domenico [1 ]
机构
[1] Univ Palermo, Dept Biol Chem & Pharmaceut Sci & Technol STEBICEF, Med Chem & Pharmaceut Technol Sect, Via Archirafi 32, I-90123 Palermo, Italy
[2] Univ Palermo, Dept Earth & Marine Sci DiSTeM, Viale Sci Ed 16, I-90128 Palermo, Italy
[3] Univ Palermo, Dept Biol Chem & Pharmaceut Sci & Technol STEBICEF, Lab Biochem, I-90127 Palermo, Italy
[4] Univ Palermo, Inst Biochem, Dept Biomed Neurosci & Adv Diagnost BIND, I-90127 Palermo, Italy
关键词
4-cinnamamido-(1H-pyrazol-5-yl)benzamides; 2-phenoxyacedamido-(1H-pyrazol-5-yl)benzamides; Antiproliferative activity; Antimicrobial activity; Antibiofilm activity; Biofilm associated infections Candida albicans; BIOLOGICAL EVALUATION; MECHANISM; DERIVATIVES; BEARING;
D O I
10.1007/s00044-024-03224-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Several new synthesized 4-cinnamamido- and 2-phenoxyacedamido-(1H-pyrazol-5-yl)benzamides were obtained by two multi step different synthetic routes in order to maximize their yield. The new derivatives were screened to determine the antiproliferative, antimicrobial and antibiofilm activity. The biological results showed how, respect to the antiproliferative and antimicrobial activities, the compounds have a low to missing activity. Different are the results obtained concerning the antibiofilm activity, especially towards Candida albicans. Most of the synthesized compounds showed a good percentage inhibition of biofilm formation ranging from 60 to 73% with a Biofilm Inhibition Concentration 50% (BIC50) from 0.13 to 0.01 mu M. Among the synthesized compounds the ethyl 5-(4-(2-(4-chlorophenoxy)acetamido)benzamido)-1-methyl-1H-pyrazole-4-carboxylate (27c) resulted the most active molecule with a BIC50 of 0.01 mu M. According to the results obtained, such compound could be considered a lead subject of further studies to obtain novel and more effective antibiofilm agents against C. albicans.
引用
收藏
页码:903 / 917
页数:15
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