scholarly journals Synthesis and antibacterial activity of monocyclic 3-carboxamide tetramic acids

2013 ◽  
Vol 9 ◽  
pp. 1899-1906 ◽  
Author(s):  
Yong-Chul Jeong ◽  
Mark G Moloney
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Chemical Library ◽  
Rapid Construction ◽  
Tetramic Acids

A chemical library of carboxamide-substituted tetramates designed by analogy with antibacterial natural products, a method for their rapid construction, and the evaluation of their antibacterial activity is reported.

Rapid construction of the 6/6/5 tricyclic framework via a tandem radical cyclization reaction and its application to the synthesis of 5-epi-7-deoxy-isoabietenin A

2017 ◽  
Vol 4 (11) ◽  
pp. 2211-2215 ◽  
Author(s):  
Hao Zhang ◽  
Shiqiang Ma ◽  
Zhimin Xing ◽  
Lin Liu ◽  
Bowen Fang ◽  
...  
Keyword(s):  
Natural Products ◽  
Radical Cyclization ◽  
Cyclization Reaction ◽  
Rapid Construction

A tandem radical cyclization towards the 6/6/5 tricyclic skeleton, which exists in numerous natural products, was developed in modest to good yields.

scholarly journals Heronapyrrole D: A case of co-inspiration of natural product biosynthesis, total synthesis and biodiscovery

2014 ◽  
Vol 10 ◽  
pp. 1228-1232 ◽  
Author(s):  
Jens Schmidt ◽  
Zeinab Khalil ◽  
Robert J Capon ◽  
Christian B W Stark
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Total Synthesis ◽  
Asymmetric Synthesis ◽  
Natural Product ◽  
Joint Effort ◽  
Natural Product Biosynthesis ◽  
New Members ◽  
Degree Of Oxidation ◽  
Rare Class

The heronapyrroles A–C have first been isolated from a marine-derived Streptomyces sp. (CMB-0423) in 2010. Structurally, these natural products feature an unusual nitropyrrole system to which a partially oxidized farnesyl chain is attached. The varying degree of oxidation of the sesquiterpenyl subunit in heronapyrroles A–C provoked the hypothesis that there might exist other hitherto unidentified metabolites. On biosynthetic grounds a mono-tetrahydrofuran-diol named heronapyrrole D appeared a possible candidate. We here describe a short asymmetric synthesis of heronapyrrole D, its detection in cultivations of CMB-0423 and finally the evaluation of its antibacterial activity. We thus demonstrate that biosynthetic considerations and the joint effort of synthetic and natural product chemists can result in the identification of new members of a rare class of natural products.

scholarly journals Potentially Effective and Safe Anti-Helicobacter pylori Natural Products: Chemometric Study

2020 ◽  
Vol 71 (6) ◽  
pp. 267-273 ◽  
Author(s):  
Branislava D. Kocic ◽  
Dobrila M. Stankovic Dordevic ◽  
Marija V. Dimitrijevic ◽  
Marija S. Markovic ◽  
Dragoljub L. Miladinovic
Keyword(s):  
Helicobacter Pylori ◽  
Antibacterial Activity ◽  
Natural Products ◽  
Chemical Composition ◽  
Essential Oils ◽  
Principal Component ◽  
Synergistic Activity ◽  
Agglomerative Hierarchical Clustering ◽  
Naturally Occurring ◽  
H Pylori

The susceptibility of Helicobacter pylori to three essential oils (EOs), 12 naturally occurring monoterpene hydrocarbons, oxygenated and phenolic monoterpenes and three reference antibiotics were studied. Classification and comparison of essential oils and monoterpenes on the basis of their chemical composition and antibacterial activity were made by the utilization of principal component analyses (PCA) and agglomerative hierarchical clustering (AHC). The most abundant compound in the Thymus glabrescens Willd. and Thymus pulegioides L. EOs is geraniol (33.8% and 52.5%), while the main constituent in Satureja kitaibelii Wierzb. ex Heuff. EO is limonene (16,1%). The compound that was the most active against H. pylori was carvacrol. EOs of T. glabrescens and S. kitaibelii exhibit higher antibacterial ability in comparison with all monoterpenes, except carvacrol, probably based on the concept of synergistic activity of essential oil components. PCA separated essential oils based on chemical composition and explain 96.5% of the total variance in the first two principal components. Essential oils, phenolic monoterpenes and two antibiotics were classified in the same sub-cluster within AHC analyses. EOs of T. glabrescens and S. kitaibelii can be used to treat infections caused by H. pylori, as a potentially effective, cheap and safe natural products. Further research of antibacterial activity of selected monoterpenes, essential oils and standard antibiotic combinations, as well as clinical study are required.

scholarly journals Bioactivity of Spongian Diterpenoid Scaffolds from the Antarctic Sponge Dendrilla antarctica

Marine Drugs ◽  
2020 ◽  
Vol 18 (6) ◽  
pp. 327 ◽  
Author(s):  
Alexandre Bory ◽  
Andrew J. Shilling ◽  
Jessie Allen ◽  
Ala Azhari ◽  
Alison Roth ◽  
...  
Keyword(s):  
Infectious Disease ◽  
Natural Products ◽  
Leishmania Donovani ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Chemical Library ◽  
Single Digit ◽  
Liver Stage ◽  
New Compounds ◽  
The Antarctic ◽  
Small Chemical

The Antarctic sponge Dendrilla antarctica is rich in defensive terpenoids with promising antimicrobial potential. Investigation of this demosponge has resulted in the generation of a small chemical library containing diterpenoid secondary metabolites with bioactivity in an infectious disease screening campaign focused on Leishmania donovani, Plasmodium falciparum, and methicillin-resistant Staphylococcus aureus (MRSA) biofilm. In total, eleven natural products were isolated, including three new compounds designated dendrillins B–D (10–12). Chemical modification of abundant natural products led to three semisynthetic derivatives (13–15), which were also screened. Several compounds showed potency against the leishmaniasis parasite, with the natural products tetrahydroaplysulphurin-1 (4) and dendrillin B (10), as well as the semisynthetic triol 15, displaying single-digit micromolar activity and low mammalian cytotoxicity. Triol 15 displayed the best profile against the liver-stage malaria parasites, while membranolide (5) and dendrillin C (11) were strong hits against MRSA biofilm cultures.

scholarly journals Eugenia uniflora L.: potential uses as a bioactive plant

2018 ◽  
Vol 85 (0) ◽  
Author(s):  
Gabriela Silva Moura ◽  
Ivan Júnior de Oliveira ◽  
Lisandro Tomas da Silva Bonome ◽  
Gilmar Franzener
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Antibacterial Activity ◽  
Natural Products ◽  
Total Phenolics ◽  
Antioxidant Compounds ◽  
Review Of The Literature ◽  
Bioactive Substances ◽  
Eugenia Uniflora

ABSTRACT: Natural products extracted from plants have always played an important role in the discovery of bioactive substances. This work carried out a review of the literature on the bioactive activities of Eugenia uniflora L. (Surinam cherries), as a potential plant in the various uses, be it medicinal, antimicrobial, antioxidant, insecticide and protective. In the literature, studies were found to confirm the antibacterial activity of E. uniflora leaves extract on Streptococcus, Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. The presence of antioxidant compounds as total phenolics, such as anthocyanins and flavonoids, induction in the protection of plants by phytoalexins, as well as insecticidal and anthelmintic effects by the use of the extract of the E. uniflora tree. Although these different potential biotics of E. uniflora have already been reported, further studies are still needed on the use of natural products extracted from E. uniflora for employment for different purposes.

scholarly journals The psychotrimine natural products have antibacterial activity against Gram-positive bacteria and act via membrane disruption

2010 ◽  
Vol 63 (11) ◽  
pp. 685-687 ◽  
Author(s):  
Mark A Schallenberger ◽  
Timothy Newhouse ◽  
Phil S Baran ◽  
Floyd E Romesberg
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Membrane Disruption ◽  
Gram Positive ◽  
Gram Positive Bacteria

Isolation of sterols from the marine fungus Corollospora lacera

2004 ◽  
Vol 50 (12) ◽  
pp. 1069-1072 ◽  
Author(s):  
Sabrena E MacKenzie ◽  
G Soundari Gurusamy ◽  
Adam Piórko ◽  
Douglas B Strongman ◽  
Tingmo Hu ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Chromatographic Separation ◽  
Prince Edward Island ◽  
Marine Fungi ◽  
Marine Fungus ◽  
Extraction Procedures ◽  
Ethylhexyl Phthalate ◽  
Weak Antibacterial Activity

Several marine fungi collected from the waters of Prince Edward Island, Canada, were screened for the presence of natural products exhibiting antibacterial activity. Both broths and mycelia of these fungi were studied using the bioassay-guided chromatographic separation. The 4 fractions from the extract of mycelia of Corollospora lacera exhibited weak antibacterial activity and were analyzed further. From these fractions, 2 sterols (5α,8α-epidioxyergosterol and 22E,24R-ergosta-7,22-diene-3β,5α,6β-triol) and a 3:1 mixture of linoleic and oleic acids were isolated. The presence of ergosterol was confirmed in dichloromethane extracts of mycelia of every fungus in this study and this sterol was isolated from the extract of mycelium of Corollospora lacera. Two other known compounds (5-hydroxymethylfuran-2-carbaldehyde and bis(2-ethylhexyl) phthalate), were isolated from the dichloromethane extract of mycelium of Monodictys pelagica. The phthalate was reported in the literature as a metabolite isolated from the fungi, but in our study it was proven to be an artifact of the culturing and (or) extraction procedures rather than a true fungal metabolite.Key words: marine fungus, sterols, metabolites.

scholarly journals Synthesis and in vitro Antibacterial Activity of Quaternization 10-Methoxycanthin-6-one Derivatives

2019 ◽  
Author(s):  
Na Li ◽  
Jiang-Kun Dai ◽  
Dan Liu ◽  
Jin-Yi Wang ◽  
Jun-Ru Wang
Keyword(s):  
Antibacterial Activity ◽  
Natural Products ◽  
Minimum Inhibitory Concentration ◽  
Pathogenic Bacteria ◽  
Antibacterial Agents ◽  
Inhibitory Concentration ◽  
Dilution Method ◽  
In Vitro Antibacterial Activity

Natural products are an important source of antibacterial agents. Canthin-6-one alkaloids have displayed potential antibacterial activity based on our previous work. In order to improve the activity, twenty-two new 3-N-benzylated 10-methoxy canthin-6-ones were designed and synthesized through quaternization reaction. The in vitro antibacterial activity against three bacteria was evaluated by double dilution method. Four compounds (6f, 6i, 6p and 6t) displayed 2-fold superiority (minimum inhibitory concentration (MIC) = 3.91 µg/mL) against agricultural pathogenic bacteria R. solanacearum and P. syringae than agrochemical propineb. Moreover, the structure–activity relationships (SARs) were also carefully summarized in order to guide the development of antibacterial canthin-6-one agents.

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