Synthesis of a Series of Chalcones and Related Flavones and Evaluation of their Antibacterial and Antifungal

被引：16

作者：

Benouda, Hind ^{[1
]}

Bouchal, Btissam ^{[2
]}

Challioui, Allal ^{[1
]}

Oulmidi, Abdelkader ^{[1
]}

Harit, Tarik ^{[1
]}

Malek, Fouad ^{[1
]}

Riahi, Abdelkhalek ^{[3
]}

Bellaoui, Mohammed ^{[2
]}

Bouammali, Boufelja ^{[1
]}

机构：

[1] Mohammed First Univ, Fac Sci, Lab Organ Chem Macromol & Nat Prod, Oujda, Morocco

[2] Mohammed First Univ, Fac Med & Pharm, Genet Unit, Oujda, Morocco

[3] Univ Reims, Grp Methodol Synth Organ, ICMR, CNRS UMR 6229, Bat Europol Agromoulin Housse,BP 1039, F-51687 Reims 2, France

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2019年 / 16卷 / 01期

关键词：

Antibacterial activity; antifungal activity; chalcones; flavones; simmons-schmidt condensation; fluconazole; ANTIMICROBIAL ACTIVITY; STAPHYLOCOCCUS-AUREUS; INFECTIONS; RESISTANCE; GALANGIN; DERIVATIVES; MECHANISM; BACTERIA; AGENTS;

D O I：

10.2174/1570180815666180404130430

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: A series of chalcones and flavones were synthesized from 2'-hydroxyacetophenone and substituted aromatic aldehydes via Simmons-Schmidt condensation followed by oxidative cyclization. Methods: Characterization of the obtained structures was established on the basis of their spectroscopic data. The synthesized compounds were screened for their antimicrobial activities against five bacterial strains (Citrobacter freundii, Staphylococcus aureus, Listeria monocytogenes, Salmonella braenderup, Escherichia coli.) and two fungal strains (Candida albicans, Candida krusei). Results: The in vitro bioassay results indicated that some target compounds displayed moderate (4d, 4e) to high (4a) antifungal activity against the pathogenic fungi C. albicans and C. krusei. Conclusion: For the antibacterial activity, only products 3d and 4d showed a weak antibacterial activity. These compounds can lead to the design of new drugs with specific antifungal activity.

引用

页码：93 / 100

页数：8

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