Design, synthesis, and biological evaluation of chrysin derivatives as potential FabH inhibitors

Li, Hongxia; Wang, Zhongchang; Qian, Yumei; Yan, Xiao; Lu, Yinan; Zhu, Hai‐Liang

doi:10.1111/cbdd.12839

Cited by 13 publications

(6 citation statements)

References 29 publications

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“…The chrysin containing morpholine compound 86 (Figure 47) displayed the most potent inhibitory activity against Escherichia coli FabH (IC 50 ¼ 5.78 ± 0.24 mM), comparing to the control positive drugs penicillin G (7.56 ± 0.30 mM). In the antibacterial activity assay, 86 was found to be the most active against S. aureus and E. coli (MIC ¼ 1.25 ± 0.01 and 1.15 ± 0.12 mg/mL, respectively), compared with the control positive drugs (MIC ¼ 1.39 ± 0.02 and 1.82 ± 0.47 mg/mL, respectively) 114 .…”

Section: Antibacterial Activitymentioning

confidence: 95%

Piperazine skeleton in the structural modification of natural products: a review

Zhang

Guo

Deng

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Piperazine moiety is a cyclic molecule containing two nitrogen atoms in positions 1 and 4, as well as four carbon atoms. Piperazine is one of the most sought heterocyclics for the development of new drug candidates with a wide range of applications. Over 100 molecules with a broad range of bioactivities, including antitumor, antibacterial, anti-inflammatory, antioxidant, and other activities, were reviewed. This article reviewed investigations regarding piperazine groups for the modification of natural product derivatives in the last decade, highlighting parameters that affect their biological activity.

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Section: Antibacterial Activitymentioning

confidence: 95%

Piperazine skeleton in the structural modification of natural products: a review

Zhang

Guo

Deng

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…aureus and E . coli with MIC values of 1.25 ± 0.01 and 1.15 ± 0.12 μg/ml, respectively (Li et al, ). Evaluation of the antibacterial activity of structural analogues of xanthohumol ( 157 ) by agar‐diffusion method revealed that chalconaringenin ( 158 ), with at least one hydroxy group at C‐4 position, demonstrated good activity.…”

Section: Synthetic Derivatives Of Flavonoidsmentioning

confidence: 99%

Antibacterial activity of flavonoids and their structure–activity relationship: An update review

Farhadi

Khameneh

Iranshahi

et al. 2018

Phytotherapy Research

390

251

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Based on World Health Organization reports, resistance of bacteria to well-known antibiotics is a major global health challenge now and in the future. Different strategies have been proposed to tackle this problem including inhibition of multidrug resistance pumps and biofilm formation in bacteria and development of new antibiotics with novel mechanism of action. Flavonoids are a large class of natural compounds, have been extensively studied for their antibacterial activity, and more than 150 articles have been published on this topic since 2005. Over the past decade, some promising results were obtained with the antibacterial activity of flavonoids. In some cases, flavonoids (especially chalcones) showed up to sixfold stronger antibacterial activities than standard drugs in the market. Some synthetic derivatives of flavonoids also exhibited remarkable antibacterial activities with 20-to 80-fold more potent activity than the standard drug against multidrug-resistant Gram-negative and Gram-positive bacteria (including Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus). This review summarizes the ever changing information on antibacterial activity of flavonoids since 2005, with a special focus on the structure-activity relationship and mechanisms of actions of this broad class of natural compounds.

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“…Although chrysin’s antimicrobial activity is less in research focus, there is some potential as chrysin inhibits viral replication [ 42 ]. In contrast, its synthetic derivatives inhibit fatty acid biosynthesis (FAB) in Escherichia coli , Pseudomonas aeruginosa , and Staphylococcus aureus [ 43 ].…”

Section: Propolis Types Key Molecules and Their Biological Activitiesmentioning

confidence: 99%

Propolis Extract and Its Bioactive Compounds—From Traditional to Modern Extraction Technologies

Šuran

Cepanec²,

Mašek

et al. 2021

Molecules

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Propolis is a honeybee product known for its antioxidant, anti-inflammatory, anticancer, and antimicrobial effects. It is rich in bioactive molecules whose content varies depending on the botanical and geographical origin of propolis. These bioactive molecules have been studied individually and as a part of propolis extracts, as they can be used as representative markers for propolis standardization. Here, we compare the pharmacological effects of representative polyphenols and whole propolis extracts. Based on the literature data, polyphenols and extracts act by suppressing similar targets, from pro-inflammatory TNF/NF-κB to the pro-proliferative MAPK/ERK pathway. In addition, they activate similar antioxidant mechanisms of action, like Nrf2-ARE intracellular antioxidant pathway, and they all have antimicrobial activity. These similarities do not imply that we should attribute the action of propolis solely to the most representative compounds. Moreover, its pharmacological effects will depend on the efficacy of these compounds’ extraction. Thus, we also give an overview of different propolis extraction technologies, from traditional to modern ones, which are environmentally friendlier. These technologies belong to an open research area that needs further effective solutions in terms of well-standardized liquid and solid extracts, which would be reliable in their pharmacological effects, environmentally friendly, and sustainable for production.

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Design, synthesis, and biological evaluation of chrysin derivatives as potential FabH inhibitors

Cited by 13 publications

References 29 publications

Piperazine skeleton in the structural modification of natural products: a review

Piperazine skeleton in the structural modification of natural products: a review

Antibacterial activity of flavonoids and their structure–activity relationship: An update review

Propolis Extract and Its Bioactive Compounds—From Traditional to Modern Extraction Technologies

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