scholarly journals New enamine derivatives of lapachol and biological activity

2002 ◽  
Vol 74 (2) ◽  
pp. 211-221 ◽  
Author(s):  
MAILCAR F. OLIVEIRA ◽  
TELMA L.G. LEMOS ◽  
MARCOS C. DE MATTOS ◽  
TACIANA A. SEGUNDO ◽  
GILVANDETE M.P. SANTIAGO ◽  
...  
Keyword(s):  
Biological Activity ◽  
Aedes Aegypti ◽  
Biological Activities ◽  
Artemia Salina ◽  
Nmr Analysis ◽  
Human Breast ◽  
Convenient Synthesis ◽  
Breast Cells ◽  
Derivatives Of

A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione, 2-(1-piperidinyl)-3-(3-methyl-2-butenyl)-1,4-naphtalenedione and 2-(1-pyrrolidinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (lapachol) and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

scholarly journals Insight into the Presence of Stilbenes in Medicinal Plants Traditionally Used in Croatian Folk Medicine

2016 ◽  
Vol 11 (6) ◽  
pp. 1934578X1601100 ◽  
Author(s):  
Ivana Generalić Mekinić ◽  
Danijela Skroza ◽  
Ivica Ljubenkov ◽  
Višnja Katalinić
Keyword(s):  
Biological Activity ◽  
Medicinal Plants ◽  
Biological Activities ◽  
Folk Medicine ◽  
Free Form ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Insight Into ◽  
Phenolic Extracts

Over the last years, great interest has arisen concerning plant stilbenes, especially resveratrol, which has a whole spectrum of positive biological activities. In this study, we investigated the presence of resveratrol monomers (trans- and cis- form) and naturally occurring derivatives of fraas-resveratrol (piceid, astringin and isorhapontin) in phenolic extracts of twenty medicinal plants traditionally used in Croatian folk medicine. The investigated compounds were present in the samples, in free form or as glucosides, and the highest share was found in immortelle, common yarrow and Lamiaceae plants. The obtained results indicate that biological activity of selected medicinal plants can be related to the presence of this valuable group of phytochemicals.

scholarly journals Chemical Composition and Biological Activities of the Black Sea Algae Polysiphonia denudata (Dillw.) Kutz. and Polysiphonia denudata f. fragilis (Sperk) Woronich

2001 ◽  
Vol 56 (11-12) ◽  
pp. 1008-1014 ◽  
Author(s):  
Salvatore De Rosa ◽  
Zornitsa Kamenarska ◽  
Vassya Bankova ◽  
Kamen Stefanov ◽  
Stefka Dimitrova-Konaklieva ◽  
...  
Keyword(s):  
Biological Activity ◽  
Chemical Composition ◽  
Black Sea ◽  
Biological Activities ◽  
Artemia Salina ◽  
Sterol Composition ◽  
The Black Sea ◽  
Polar Components

Abstract The two investigated algae had almost identical sterol composition, but there were signifi­cant differences in the com position of the polar components and especially in the composi­tion of the volatiles. P. denudata f. fragilis extracts possessed a stronger biological activity (antibacterial, antifungal and toxicity against Artemia salina). Despite the minute morpholog­ical differences between the two algae, we recommend P. denudata f. fragilis to be regarded as P. denudata subsp. fragilis.

scholarly journals Chemical Compositions and Biological Activities of Leaf Essential Oils of Twelve Species of Piper from Monteverde, Costa Rica

2008 ◽  
Vol 3 (8) ◽  
pp. 1934578X0800300 ◽  
Author(s):  
William N. Setzer ◽  
Grace Park ◽  
Brittany R. Agius ◽  
Sean L. Stokes ◽  
Tameka M. Walker ◽  
...  
Keyword(s):  
Costa Rica ◽  
Essential Oils ◽  
Biological Activities ◽  
Artemia Salina ◽  
Chemical Compositions ◽  
Human Breast ◽  
Human Breast Tumor ◽  
Leaf Oil ◽  
Mcf 7

The leaf essential oils of twelve species of Piper (Piperaceae) from Monteverde, Costa Rica ( Piper aequale, Piper amalago, Piper biasperatum, Piper bredemeyeri, Piper dotanum, Piper fimbriulatum, Piper glabrescens, Piper imperiale, Piper lanceifolium, Piper nemorense, Piper oblanceolatum, and Piper sp. A near aereum) have been obtained by hydrodistillation and analyzed by GC-MS. The Piper leaf oils have been screened for antibacterial activity against Bacillus cereus, Staphylococcus aureus, and Escherichia coli; for Artemia salina (brine shrimp) lethality; for in-vitro cytotoxic activity against MCF-7 (human breast tumor) cells; and inhibition of the cysteine protease cruzain. A cluster analysis comparison with previously published Piper leaf oil compositions was carried out in order to discern the differences and similarities between the volatile chemical compositions of Piper species.

scholarly journals Synthetic Chiral Derivatives of Xanthones: Biological Activities and Enantioselectivity Studies

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 791 ◽  
Author(s):  
Carla Fernandes ◽  
Maria Carraro ◽  
João Ribeiro ◽  
Joana Araújo ◽  
Maria Tiritan ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Pharmacological Activities ◽  
Sar Studies ◽  
Naturally Occurring ◽  
Structure Activity ◽  
Wide Range ◽  
Synthetic Methodologies ◽  
Derivatives Of ◽  
Biological And Pharmacological Activities

Many naturally occurring xanthones are chiral and present a wide range of biological and pharmacological activities. Some of them have been exhaustively studied and subsequently, obtained by synthesis. In order to obtain libraries of compounds for structure activity relationship (SAR) studies as well as to improve the biological activity, new bioactive analogues and derivatives inspired in natural prototypes were synthetized. Bioactive natural xanthones compromise a large structural multiplicity of compounds, including a diversity of chiral derivatives. Thus, recently an exponential interest in synthetic chiral derivatives of xanthones (CDXs) has been witnessed. The synthetic methodologies can afford structures that otherwise could not be reached within the natural products for biological activity and SAR studies. Another reason that justifies this trend is that both enantiomers can be obtained by using appropriate synthetic pathways, allowing the possibility to perform enantioselectivity studies. In this work, a literature review of synthetic CDXs is presented. The structures, the approaches used for their synthesis and the biological activities are described, emphasizing the enantioselectivity studies.

scholarly journals Synthesis, Modification and Biological Activity of Diosgenyl β-d-Glycosaminosides: An Overview

Molecules ◽  
2020 ◽  
Vol 25 (22) ◽  
pp. 5433
Author(s):  
Daria Grzywacz ◽  
Beata Liberek ◽  
Henryk Myszka
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Protecting Groups ◽  
Pharmacological Properties ◽  
Amino Group ◽  
Reaction Conditions ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Wide Group ◽  
Derivatives Of

Saponins are a structurally diverse class of natural glycosides that possess a broad spectrum of biological activities. They are composed of hydrophilic carbohydrate moiety and hydrophobic triterpenoid or steroid aglycon. Naturally occurring diosgenyl glycosides are the most abundant steroid saponins, and many of them exhibit various pharmacological properties. Herein, we present an overview of semisynthetic saponins syntheses–diosgenyl β-d-glycosaminosides (d-gluco and d-galacto). These glycosides possess a 2-amino group, which creates great possibilities for further modifications. A wide group of glycosyl donors, different N-protecting groups and various reaction conditions used for their synthesis are presented. In addition, this paper demonstrates the possibilities of chemical modifications of diosgenyl β-d-glycosaminosides, associated with functionalisation of the amino group. These provide N-acyl, N-alkyl, N,N-dialkyl, N-cinnamoyl, 2-ureido and 2-thiosemicarbazonyl derivatives of diosgenyl β-d-glycosaminosides, for which the results of biological activity tests (antifungal, antibacterial, anti-cancer and hemolytic) are presented.

scholarly journals Larvicidal activity, molluscicide and toxicity of the essential oil of Citrus limon peels against, respectively, Aedes aegypti, Biomphalaria glabrata and Artemia salina

2019 ◽  
Vol 44 (4) ◽  
pp. 85 ◽  
Author(s):  
Paulo Roberto Barros Gomes ◽  
Marlucy Bezerra Oliveira ◽  
Dionney Andrade De Sousa ◽  
Jeremias Caetano Da Silva ◽  
Romer Pessôa Fernandes ◽  
...  
Keyword(s):  
Essential Oil ◽  
Aedes Aegypti ◽  
Larvicidal Activity ◽  
Biological Activities ◽  
Biomphalaria Glabrata ◽  
Artemia Salina ◽  
World Health ◽  
Lethal Concentration ◽  
Major Constituent ◽  
Citrus Limon

In this present work, we tested the larvicidal activity, molluscicide and toxicity of the oil extracted from Citrus limon peels, respectively against third stage larvae of Aedes aegypti, snail Biomphalaria glabrata, and Artemia salina. For this, we extract the essential oil by hydrodistillation. Then, we identified and quantified the components by gas chromatography coupled to mass spectrometry (GC-MS). We tested the larvicidal and molluscicidal activity, respectively, using the method adopted by the Brazilian Ministry of Health and the World Health Organization. We calculated the lethal concentration (LC50) from the Probit method for the three biological activities with 95 %. The results of the chromatographic analysis showed that the oil has 58.81% of Limonene (major constituent) and 0.11% α-Mulene (minority component). The essential oil presented lethal concentration (LC50) for larvicidal activity, molluscicide and toxicity, respectively at 15.48, 13.05 and 743.35 mg∙L-1. Therefore, the essential oil is active against larvae of A. aegypti and snail B. glabrata and non-toxic against larvae of A. salina.

scholarly journals 3,4-dihydro-2H-1,3-benzoxazines and their oxo-derivatives chemistry and bioactivities

2020 ◽  
pp. 1-1 ◽  
Author(s):  
El-Din Sharaf
Keyword(s):  
Biological Activity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Significant Class

3,4-Dihydro-2H-1,3-benzoxazines derivatives are a significant class of heterocycles with a particular awareness due to their remarkable biological activities in humans, plant as well as in animals and also, they are naturally occurrence. Because of alteration in the benzoxazines skeleton, beside their comparative chemical simplicity and accessibility, make these compounds to be suitable sources of other bioactive compounds. Resulting in the discovery of a wide set of these compounds that have a broad biological activity such as antifungal, antibacterial, anti-HIV, anticancer, anticonvulsant, anti-inflammatory and so on. Subsequently, this review herein gives a brief overview of derivatives of 3,4-dihydro-2H-1,3-benzoxazines monomers and their oxo-derivatives chemistry and bioactivities.

Synthesis of Some New Derivatives of Pyrrolidine-2-one and Studying Their Antibacterial Potentials

2020 ◽  
Vol 38 (3B) ◽  
pp. 128-141
Author(s):  
Nadia A. Betti ◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Hydrazine Hydrate ◽  
1H Nmr ◽  
Mass Spectra ◽  
Biological Activities ◽  
Ft Ir ◽  
Derivatives Of ◽  
And Staphylococcus Aureus

New derivatives of pyrrolidine-2-one have been synthesized through lactamization of γ –butyrolactone (GBL) by hydrazine hydrate (80%), ethylene diamine and ethanol amine to afford compounds (1-aminopyrrolidin-2-one), (1-(2-aminoethyl)pyrrolidine-2-one) and (1-(2-hydroxyethyl)pyrrolidine-2-one), respectively. Compound (1-aminopyrrolidin-2-one) underwent several reactions to synthesize the rest of these derivatives. All synthesized compounds were approved by their FT-IR, 1H-NMR and some by Mass spectra. The biological activities of these derivatives were evaluated against Escherichia coli and Staphylococcus aureus. Many of these derivatives showed moderate biological activity against one or both kind of bacteria in comparison to amoxicillin and some showed no biological activity at all.

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