scholarly journals Rapid pseudo five-component synthesis of intensively blue luminescent 2,5-di(hetero)arylfurans via a Sonogashira–Glaser cyclization sequence

2014 ◽  
Vol 10 ◽  
pp. 672-679 ◽  
Author(s):  
Fabian Klukas ◽  
Alexander Grunwald ◽  
Franziska Menschel ◽  
Thomas J J Müller
Keyword(s):  
Natural Products ◽  
Electronic Structure ◽  
Biologically Active ◽  
Blue Luminescence ◽  
Quantum Yields ◽  
One Pot ◽  
Dft Computations ◽  
High Quantum ◽  
Bright Blue ◽  
Coupling Sequence

2,5-Di(hetero)arylfurans are readily accessible in a pseudo five-component reaction via a Sonogashira–Glaser coupling sequence followed by a superbase-mediated (KOH/DMSO) cyclization in a consecutive one-pot fashion. Besides the straightforward synthesis of natural products and biologically active molecules all representatives are particularly interesting due to their bright blue luminescence with remarkably high quantum yields. The electronic structure of the title compounds is additionally studied with DFT computations.

Synthesis and Photophysical Properties of 1,4-Dihydro-2H,5H-chromeno[4,3-d][1,3]oxazin-5-ones, and Derivatives Containing Tethered 1,2,3-Triazoles, from 4-Aminocoumarins

Synthesis ◽  
2019 ◽  
Vol 51 (15) ◽  
pp. 2965-2976
Author(s):  
Marina C. Dilelio ◽  
Nathan P. Brites ◽  
Larissa A. Vieira ◽  
Bernardo A. Iglesias ◽  
Teodoro S. Kaufman ◽  
...  
Keyword(s):  
Nitrogen Atom ◽  
Click Chemistry ◽  
Photophysical Properties ◽  
Quantum Yields ◽  
One Pot ◽  
Alkyl Aryl ◽  
Triazole Derivatives ◽  
High Quantum ◽  
Stokes Shifts

A facile protocol for the unprecedented one-pot H2SO4-mediated hydroxymethylation/cyclative N,O-acetalization of 4-aminocoumarins to 1,4-dihydro-2H,5H-chromeno[4,3-d][1,3]oxazin-5-ones, in moderate to good yields, was developed and optimized. The scope and limitations of the transformation, which takes place in water or water/THF mixtures, were also studied. The nitrogen atom of the resulting tricycles was used to tether alkyl, aryl and 1,2,3-triazolylmethyl moieties, employing a two-step click chemistry approach for the latter. The photophysical properties of the heterocycles, as well as of their 1,2,3-triazole derivatives, were also examined. The N-aryl derivatives exhibited high quantum yields of fluorescence (up to Φf = 0.69) and very large Stokes shifts (up to 201 nm).

Domino and one-pot syntheses of biologically active compounds using diphenylprolinol silyl ether

2020 ◽  
Vol 5 (6) ◽  
Author(s):  
Yujiro Hayashi
Keyword(s):  
Natural Products ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Silyl Ether ◽  
One Pot ◽  
Active Compounds

AbstractThe successful application of diphenylprolinol silyl ether, which is one of the widely used organocatalysts, to the synthesis of natural products and drugs, is described mostly focusing on the author’s results. The molecules that are explained in this paper are baclofen, telcagepant, oseltamivir, ABT-341, prostaglandins, estradiol, horsfiline and coerulescine.

Rhodium-Catalyzed Double Isocyanide Insertion via a Vinylcarbodiimide Intermediate for the Synthesis of 2H-Pyrrol-2-imines

Synthesis ◽  
2019 ◽  
Vol 51 (17) ◽  
pp. 3250-3258
Author(s):  
Yunlong Wang ◽  
Zongyang Li ◽  
Haiying Zhao ◽  
Zhenhua Zhang
Keyword(s):  
Natural Products ◽  
Cascade Reaction ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Structural Motif ◽  
One Pot ◽  
Active Compounds

2H-Pyrrol-2-imine is an important structural motif exhibiting in biologically active compounds and natural products. An efficient rhodium-catalyzed one-pot reaction of one vinyl azide with sequentially with two different isocyanides is reported, which offers an alternative facile access to 3-amino-5-aryl-2H-pyrrol-2-imines bearing various substitution on the nitrogens in good yields. An unstable vinylcarbodiimide is the key intermediate in this cascade reaction.

Biologically active natural products from Cassine viburnifolia

Planta Medica ◽  
2015 ◽  
Vol 81 (11) ◽  
Author(s):  
T Grkovic ◽  
R Akee ◽  
J Evans ◽  
JM Collins ◽  
B O'Keefe
Keyword(s):  
Natural Products ◽  
Biologically Active ◽  
Active Natural

Recent Progress Towards Synthesis of the Indolizidine Alkaloid 195B

2020 ◽  
Vol 17 (2) ◽  
pp. 82-90 ◽  
Author(s):  
Ghodsi Mohammadi Ziarani ◽  
Fatemeh Mohajer ◽  
Zohreh kheilkordi
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Recent Progress ◽  
Human Life ◽  
Natural Compounds ◽  
Biologically Active ◽  
Pharmaceutical Chemistry ◽  
Biological Perspective ◽  
Highly Active

Background: Natural products have been received attention due to their importance in human life as those are biologically active. In this review, there are some reports through different methods related to the synthesis of the indolizidine 195B which was extracted from poisonous frog; however, due to respect nature, the synthesis of natural compounds such as indolizidine has been attracted much attention among scientists and researchers. Objective: This review discloses the procedures and methods to provide indolizidine 195B from 1989 to 2018 due to their importance as a natural product. Conclusion: There are several methods to give rise to the indolizidine 195B as a natural product that is highly active from the biological perspective in pharmaceutical chemistry. In summary, many protocols for the preparations of indolizidine 195B from various substrates, several reagents, and conditions have been reported from different aromatic and aliphatic.

A Facile One-Pot Synthesis of 3-Methylbenzisoxazoles via a Key Intermediate of ortho-Ethoxyvinyl Nitroaryls by Domino Rearrangement and Their Anti- Inflammatory Activity

2020 ◽  
Vol 16 (8) ◽  
pp. 1161-1165
Author(s):  
Bashetti Nagaraju ◽  
Jagarlapudi V. Shanmukhakumar ◽  
Nareshvarma Seelam ◽  
Tondepu Subbaiah ◽  
Bethanamudi Prasanna
Keyword(s):  
Stannous Chloride ◽  
Biologically Active ◽  
Inflammatory Activity ◽  
Albino Rats ◽  
One Pot ◽  
Simple Method ◽  
Standard Drug ◽  
Entire Study ◽  
One Pot Synthesis ◽  
Anti Inflammatory

Background: Recently, there has been a lot of scientific interest in exploring the syntheses of oxygen and nitrogen-containing heterocyclic compounds due to their pharmacological activities. In addition, benzisoxazoles play a very important role in organic synthesis as key intermediates. Objective: In this paper, we focused on developing a novel synthetic route for biologically active arylisoxazoles under normal conditions, and simplified it to get high purities and yields, and also reported their anti-inflammatory activities. Method: An efficient and simple method has been explored for the synthesis of novel 3-methyl arylisoxazoles from o-nitroaryl halides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via Domino rearrangement in one pot synthesis. Result: We synthesized novel 3-methylarylisoxazoles from o-nitroarylhalides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via domino rearrangement. In this reduction, nitro group and ethoxy vinyl group change to the functional acyl ketones, followed by hetero cyclization. Here, the reaction proceeds without the isolation of intermediates like 2-acylnitroarenes and 2- acylanilines. All the synthesized compounds were completely characterized by the NMR and mass spectra. The compounds were also explored for their anti-inflammatory activity by carrageenan-induced inflammation in the albino rats (150-200 g) of either sex used in this entire study with the use of Diclofenac sodium as the standard drug. The initial evaluations identified leading targets with good to moderate anti-inflammatory activity. Conclusion: A simple, one-pot and convenient method has been explored for the synthesis of novel 3- methylarylisoxazoles with high purity and reaction yields. All the compounds 3a, 3c, 3d, 3f, 3g and 3h exhibited 51-64% anti-inflammatory activities.

scholarly journals Facile Bio-Fabrication of Ag-Cu-Co Trimetallic Nanoparticles and Its Fungicidal Activity against Candida auris

2021 ◽  
Vol 7 (1) ◽  
pp. 62 ◽  
Author(s):  
Majid Rasool Kamli ◽  
Vartika Srivastava ◽  
Nahid H. Hajrah ◽  
Jamal S. M. Sabir ◽  
Khalid Rehman Hakeem ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Antimicrobial Properties ◽  
Bloodstream Infections ◽  
Multidrug Resistant ◽  
Biologically Active ◽  
Phase Cell ◽  
Candida Auris ◽  
Medical Problems ◽  
One Pot ◽  
X Ray

Candida auris is an emergent multidrug-resistant pathogen that can lead to severe bloodstream infections associated with high mortality rates, especially in hospitalized individuals suffering from serious medical problems. As Candida auris is often multidrug-resistant, there is a persistent demand for new antimycotic drugs with novel antifungal action mechanisms. Here, we reported the facile, one-pot, one-step biosynthesis of biologically active Ag-Cu-Co trimetallic nanoparticles using the aqueous extract of Salvia officinalis rich in polyphenols and flavonoids. These medicinally important phytochemicals act as a reducing agent and stabilize/capping in the nanoparticles’ fabrication process. Fourier Transform-Infrared, Scanning electron microscopy, Transmission Electron Microscopy, Energy dispersive X-Ray, X-ray powder diffraction and Thermogravimetric analysis (TGA) measurements were used to classify the as-synthesized nanoparticles. Moreover, we evaluated the antifungal mechanism of as-synthesized nanoparticles against different clinical isolates of C. auris. The minimum inhibitory concentrations and minimum fungicidal concentrations ranged from 0.39–0.78 μg/mL and 0.78–1.56 μg/mL. Cell count and viability assay further validated the fungicidal potential of Ag-Cu-Co trimetallic nanoparticles. The comprehensive analysis showed that these trimetallic nanoparticles could induce apoptosis and G2/M phase cell cycle arrest in C. auris. Furthermore, Ag-Cu-Co trimetallic nanoparticles exhibit enhanced antimicrobial properties compared to their monometallic counterparts attributed to the synergistic effect of Ag, Cu and Co present in the as-synthesized nanoparticles. Therefore, the present study suggests that the Ag-Cu-Co trimetallic nanoparticles hold the capacity to be a lead for antifungal drug development against C. auris infections.

scholarly journals Natural Products from Tongan Marine Organisms

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4534
Author(s):  
Taitusi Taufa ◽  
Ramesh Subramani ◽  
Peter Northcote ◽  
Robert Keyzers
Keyword(s):  
Natural Products ◽  
Pacific Ocean ◽  
Biological Activities ◽  
Marine Sponges ◽  
Marine Organisms ◽  
Biologically Active ◽  
Geographic Variability ◽  
South Pacific Ocean ◽  
New Novel ◽  
Rich Diversity

The islands of the South Pacific Ocean have been in the limelight for natural product biodiscovery, due to their unique and pristine tropical waters and environment. The Kingdom of Tonga is an archipelago in the central Indo-Pacific Ocean, consisting of 176 islands, 36 of which are inhabited, flourishing with a rich diversity of flora and fauna. Many unique natural products with interesting bioactivities have been reported from Indo-Pacific marine sponges and other invertebrate phyla; however, there have not been any reviews published to date specifically regarding natural products from Tongan marine organisms. This review covers both known and new/novel Marine Natural Products (MNPs) and their biological activities reported from organisms collected within Tongan territorial waters up to December 2020, and includes 109 MNPs in total, the majority from the phylum Porifera. The significant biological activity of these metabolites was dominated by cytotoxicity and, by reviewing these natural products, it is apparent that the bulk of the new and interesting biologically active compounds were from organisms collected from one particular island, emphasizing the geographic variability in the chemistry between these organisms collected at different locations.

Sign in / Sign up

Export Citation Format

Share Document