scholarly journals Correction: Surowiak, A.K.; Lochyński, S.; Strub, D.J. Unsubstituted Oximes as Potential Therapeutic Agents. Symmetry 2020, 12, 575

Symmetry ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 1006
Author(s):  
Alicja K. Surowiak ◽  
Stanisław Lochyński ◽  
Daniel J. Strub
Keyword(s):  
Biological Activity ◽  
Adjuvant Therapy ◽  
Chemical Synthesis ◽  
Carbonyl Compounds ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Anticancer Activities ◽  
Medical Sector ◽  
Cancer And Inflammation ◽  
Increased Activity

Oximes, which are highly bioactive molecules, have versatile uses in the medical sector and have been indicated to possess biological activity. Certain oximes exist in nature in plants and animals, but they are also obtained by chemical synthesis. Oximes are known for their anti-inflammatory, antimicrobial, antioxidant and anticancer activities. Moreover, they are therapeutic agents against organophosphate (OP) poisoning. Two oximes are already commonly used in therapy. Due to these abilities, new oxime compounds have been synthesized, and their biological activity has been verified. Often, modification of carbonyl compounds into oximes leads to increased activity. Nevertheless, in some cases, oxime activity is connected to the activity of the substrate. Recent works have revealed that new oxime compounds can demonstrate such functions and thus are considered to be potential drugs for pathogenic diseases, as adjuvant therapy in various types of cancer and inflammation and as potential next-generation drugs against OP poisoning.

scholarly journals Unsubstituted Oximes as Potential Therapeutic Agents

Symmetry ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 575 ◽  
Author(s):  
Alicja K. Surowiak ◽  
Stanisław Lochyński ◽  
Daniel J. Strub
Keyword(s):  
Biological Activity ◽  
Adjuvant Therapy ◽  
Chemical Synthesis ◽  
Carbonyl Compounds ◽  
Therapeutic Agents ◽  
Bioactive Molecules ◽  
Anticancer Activities ◽  
Medical Sector ◽  
Cancer And Inflammation ◽  
Increased Activity

Oximes, which are highly bioactive molecules, have versatile uses in the medical sector and have been indicated to possess biological activity. Certain oximes exist in nature in plants and animals, but they are also obtained by chemical synthesis. Oximes are known for their anti-inflammatory, antimicrobial, antioxidant and anticancer activities. Moreover, they are therapeutic agents against organophosphate (OP) poisoning. Two oximes are already commonly used in therapy. Due to these abilities, new oxime compounds have been synthesized, and their biological activity has been verified. Often, modification of carbonyl compounds into oximes leads to increased activity. Nevertheless, in some cases, oxime activity is connected to the activity of the substrate. Recent works have revealed that new oxime compounds can demonstrate such functions and thus are considered to be potential drugs for pathogenic diseases, as adjuvant therapy in various types of cancer and inflammation and as potential next-generation drugs against OP poisoning.

Natural Compounds and Drug Discovery: Can Cnidarian Venom Play a Role?

2019 ◽  
Vol 19 (2) ◽  
pp. 114-118
Author(s):  
Gian Luigi Mariottini ◽  
Irwin Darren Grice
Keyword(s):  
Biological Activity ◽  
Marine Species ◽  
Natural Compounds ◽  
Therapeutic Agents ◽  
Industrial Applications ◽  
Bioactive Molecules ◽  
Sea Anemones ◽  
Therapeutic Approaches ◽  
Ongoing Research ◽  
Biological Compounds

Natural compounds extracted from organisms and microorganisms are an important resource for the development of drugs and bioactive molecules. Many such compounds have made valuable contributions in diverse fields such as human health, pharmaceutics and industrial applications. Presently, however, research on investigating natural compounds from marine organisms is scarce. This is somewhat surprising considering that the marine environment makes a major contribution to Earth's ecosystems and consequently possesses a vast storehouse of diverse marine species. Interestingly, of the marine bioactive natural compounds identified to date, many are venoms, coming from Cnidarians (jellyfish, sea anemones, corals). Cnidarians are therefore particularly interesting marine species, producing important biological compounds that warrant further investigation for their development as possible therapeutic agents. From an experimental aspect, this review aims to emphasize and update the current scientific knowledge reported on selected biological activity (antiinflammatory, antimicrobial, antitumoral, anticoagulant, along with several less studied effects) of Cnidarian venoms/extracts, highlighting potential aspects for ongoing research towards their utilization in human therapeutic approaches.

scholarly journals Fungal Biotransformation of 2′-Methylflavanone and 2′-Methylflavone as a Method to Obtain Glycosylated Derivatives

2021 ◽  
Vol 22 (17) ◽  
pp. 9617
Author(s):  
Agnieszka Krawczyk-Łebek ◽  
Monika Dymarska ◽  
Tomasz Janeczko ◽  
Edyta Kostrzewa-Susłow
Keyword(s):  
Biological Activity ◽  
Nmr Spectroscopy ◽  
Chemical Synthesis ◽  
Filamentous Fungi ◽  
Aqueous Solubility ◽  
Isaria Fumosorosea ◽  
Valuable Method ◽  
Biotransformation Products ◽  
Pharmaceutical Agents ◽  
Increased Activity

Methylated flavonoids are promising pharmaceutical agents due to their improved metabolic stability and increased activity compared to unmethylated forms. The biotransformation in cultures of entomopathogenic filamentous fungi is a valuable method to obtain glycosylated flavones and flavanones with increased aqueous solubility and bioavailability. In the present study, we combined chemical synthesis and biotransformation to obtain methylated and glycosylated flavonoid derivatives. In the first step, we synthesized 2′-methylflavanone and 2′-methylflavone. Afterwards, both compounds were biotransformed in the cultures of two strains of entomopathogenic filamentous fungi Beauveria bassiana KCH J1.5 and Isaria fumosorosea KCH J2. We determined the structures of biotransformation products based on NMR spectroscopy. Biotransformations of 2′-methyflavanone in the culture of B. bassiana KCH J1.5 resulted in three glycosylated flavanones: 2′-methylflavanone 6-O-β-d-(4″-O-methyl)-glucopyranoside, 3′-hydroxy-2′-methylflavanone 6-O-β-d-(4″-O-methyl)-glucopyranoside, and 2-(2′-methylphenyl)-chromane 4-O-β-d-(4″-O-methyl)-glucopyranoside, whereas in the culture of I. fumosorosea KCH J2, two other products were obtained: 2′-methylflavanone 3′-O-β-d-(4″-O-methyl)-glucopyranoside and 2-methylbenzoic acid 4-O-β-d-(4′-O-methyl)-glucopyranoside. 2′-Methylflavone was effectively biotransformed only by I. fumosorosea KCH J2 into three derivatives: 2′-methylflavone 3′-O-β-d-(4″-O-methyl)-glucopyranoside, 2′-methylflavone 4′-O-β-d-(4″-O-methyl)-glucopyranoside, and 2′-methylflavone 5′-O-β-d-(4″-O-methyl)-glucopyranoside. All obtained glycosylated flavonoids have not been described in the literature until now and need further research on their biological activity and pharmacological efficacy as potential drugs.

A FACILE SYNTHESIS AND REACTIONS OF AMINO SELENOLO[2,3-b]PYRIDINE CARBOXYLATE

2015 ◽  
Vol 12 (1) ◽  
pp. 3910-3918 ◽  
Author(s):  
Dr Remon M Zaki ◽  
Prof Adel M. Kamal El-Dean ◽  
Dr Nermin A Marzouk ◽  
Prof Jehan A Micky ◽  
Mrs Rasha H Ahmed
Keyword(s):  
Biological Activity ◽  
Carbonyl Compounds ◽  
Mass Spectra ◽  
The Other ◽  
Pyridine Derivatives ◽  
Facile Synthesis ◽  
High Biological Activity ◽  
Basic Hydrolysis ◽  
Pyridine Carboxylate ◽  
Hydrolysis Of

 Incorporating selenium metal bonded to the pyridine nucleus was achieved by the reaction of selenium metal with 2-chloropyridine carbonitrile 1 in the presence of sodium borohydride as reducing agent. The resulting non isolated selanyl sodium salt was subjected to react with various α-halogenated carbonyl compounds to afford the selenyl pyridine derivatives 3a-f  which compounds 3a-d underwent Thorpe-Ziegler cyclization to give 1-amino-2-substitutedselenolo[2,3-b]pyridine compounds 4a-d, while the other compounds 3e,f failed to be cyclized. Basic hydrolysis of amino selenolo[2,3-b]pyridine carboxylate 4a followed by decarboxylation furnished the corresponding amino selenolopyridine compound 6 which was used as a versatile precursor for synthesis of other heterocyclic compound 7-16. All the newly synthesized compounds were established by elemental and spectral analysis (IR, 1H NMR) in addition to mass spectra for some of them hoping these compounds afforded high biological activity.

Synthesis and Biological Activity Study of Tanshinone Derivatives: A Literature and Patent Review

2020 ◽  
Vol 20 (28) ◽  
pp. 2520-2534
Author(s):  
He Huang ◽  
Chuanjun Song ◽  
Junbiao Chang
Keyword(s):  
Biological Activity ◽  
Herbal Medicine ◽  
Chemical Synthesis ◽  
Bioactive Compounds ◽  
Chinese Herbal Medicine ◽  
Salvia Miltiorrhiza ◽  
Salvia Miltiorrhiza Bunge ◽  
Chinese Herbal ◽  
Patent Review

: Tanshinones are a class of bioactive compounds present in the Chinese herbal medicine Danshen (Salvia miltiorrhiza Bunge), containing among others, abietane diterpene quinone scaffolds. Chemical synthesis and biological activity studies of natural and unnatural tanshinone derivatives have been reviewed in this article.

Synthesis of New α-Amino Phosphonates Containing 3-Amino-4(3H) Quinazolinone Moiety as Anticancer and Antimicrobial Agents: DFT, NBO, and Vibrational Studies

2018 ◽  
Vol 15 (2) ◽  
pp. 286-296 ◽  
Author(s):  
Mohamed K. Awad ◽  
Mahmoud F. Abdel-Aal ◽  
Faten M. Atlam ◽  
Hend A. Hekal
Keyword(s):  
Biological Activity ◽  
Cell Line ◽  
Quantum Chemical ◽  
Density Functional ◽  
Carcinoma Cell ◽  
Liver Carcinoma ◽  
Anticancer Activities ◽  
Functional Theory ◽  
Ft Ir ◽  
Good Agreement

Aim and Objective: Synthesis of new .-aminophosphonates containing quinazoline moiety through Kabachnik-Fields reaction in the presence of copper triflate catalyst [32], followed by studying their antimicrobial activities and in vitro anticancer activities against liver carcinoma cell line (HepG2) with the hope that new anticancer agents could be developed. Also, the quantum chemical calculations are performed using density functional theory (DFT) to study the effect of the changes of molecular and electronic structures on the biological activity of the investigated compounds. Materials and Method: The structures of the synthesized compounds are confirmed by FT-IR, 1H NMR, 13C NMR, 31P NMR and MS spectral data. The synthesized compounds show significant antimicrobial and also remarkable cytotoxicity anticancer activities against liver carcinoma cell line (HepG2). Density functional theory (DFT) was performed to study the effect of the molecular and electronic structure changes on the biological activity. Results: It was found that the electronic structure of the substituents affects on the reaction yield. The electron withdrawing substituent, NO2 group 3b, on the aromatic aldehydes gave a good yield more than the electron donating substituent, OH group 3c. The electron deficient on the carbon atom of the aldehydic group may increase the interaction of the Lewis acid (Cu(OTf)2) and the Lewis base (imine nitrogen), and accordingly, facilitate the formation of imine easily, which is attacked by the nucleophilic phosphite species to give the α- aminophosphonates. Conclusion: The newly synthesized compounds exhibit a remarkable inhibition of the growth of Grampositive, Gram-negative bacteria and fungi at low concentrations. The cytotoxicity of the synthesized compounds showed a significant cytotoxicity against the liver cancer cell line (HepG 2). Also, it was shown from the quantum chemical calculations that the electron-withdrawing substituent increases the biological activity of the α-aminophosphonates more than the electron donating group which was in a good agreement with the experimental results. Also, a good agreement between the experimental FT-IR and the calculated one was found.

scholarly journals Enantioselective Catalytic C-H Amidations: An Highlight

Catalysts ◽  
2021 ◽  
Vol 11 (4) ◽  
pp. 471
Author(s):  
Eleonora Tosi ◽  
Renata Marcia de Figueiredo ◽  
Jean-Marc Campagne
Keyword(s):  
Biological Activity ◽  
Chemical Synthesis ◽  
Crucial Role ◽  
Medicinal Chemistry ◽  
Life Sciences ◽  
Biological Processes ◽  
Chiral Molecules ◽  
Material Sciences ◽  
Innovative Approaches

The crucial role played by compounds bearing amide functions, not only in biological processes but also in several fields of chemistry, life polymers and material sciences, has brought about many significant discoveries and innovative approaches for their chemical synthesis. Indeed, a plethora of strategies has been developed to reach such moieties. Amides within chiral molecules are often associated with biological activity especially in life sciences and medicinal chemistry. In most of these cases, their synthesis requires extensive rethinking methodologies. In the very last years (2019–2020), enantioselective C-H functionalization has appeared as a straightforward alternative to reach chiral amides. Therein, an overview on these transformations within this timeframe is going to be given.

scholarly journals Cordycepin analogues of 2-5A and its derivatives. Chemical synthesis and biological activity.

1983 ◽  
Vol 258 (3) ◽  
pp. 1671-1677
Author(s):  
H Sawai ◽  
J Imai ◽  
K Lesiak ◽  
M I Johnston ◽  
P F Torrence
Keyword(s):  
Biological Activity ◽  
Chemical Synthesis

scholarly journals Kinetic resolution of indolines by asymmetric hydroxylamine formation

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Gang Wang ◽  
Ran Lu ◽  
Chuangchuang He ◽  
Lei Liu
Keyword(s):  
Hydrogen Peroxide ◽  
Chemical Synthesis ◽  
Late Stage ◽  
Kinetic Resolution ◽  
High Efficiency ◽  
Bond Formation ◽  
Bioactive Molecules ◽  
Environmentally Benign ◽  
Secondary Amines

AbstractCatalytic kinetic resolution of amines represents a longstanding challenge in chemical synthesis. Here, we described a kinetic resolution of secondary amines through oxygenation to produce enantiopure hydroxylamines involving N–O bond formation. The economic and practical titanium-catalyzed asymmetric oxygenation with environmentally benign hydrogen peroxide as oxidant is applicable to a range of racemic indolines with multiple stereocenters and diverse substituent patterns in high efficiency with efficient chemoselectivity and enantio-discrimination. Late-stage asymmetric oxygenation of bioactive molecules that are otherwise difficult to synthesize was also explored.

scholarly journals Phytochemicals and Biological Activity of Desert Date (Balanites aegyptiaca (L.) Delile)

Plants ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 32
Author(s):  
Hosakatte Niranjana Murthy ◽  
Guggalada Govardhana Yadav ◽  
Yaser Hassan Dewir ◽  
Abdullah Ibrahim
Keyword(s):  
Biological Activity ◽  
Middle East ◽  
Bioactive Compounds ◽  
Phenolic Acids ◽  
Tree Species ◽  
Indian Subcontinent ◽  
Therapeutic Agents ◽  
Root Bark ◽  
Balanites Aegyptiaca ◽  
Anti Inflammatory

Many underutilized tree species are good sources of food, fodder and possible therapeutic agents. Balanites aegyptiaca (L.) Delile belongs to the Zygophyllaceae family and is popularly known as “desert date”, reflecting its edible fruits. This tree grows naturally in Africa, the Middle East and the Indian subcontinent. Local inhabitants use fruits, leaves, roots, stem and root bark of the species for the treatment of various ailments. Several research studies demonstrate that extracts and phytochemicals isolated from desert date display antioxidant, anticancer, antidiabetic, anti-inflammatory, antimicrobial, hepatoprotective and molluscicidal activities. Mesocarp of fruits, seeds, leaves, stem and root bark are rich sources of saponins. These tissues are also rich in phenolic acids, flavonoids, coumarins, alkaloids and polysterols. Some constituents show antioxidant, anticancer and antidiabetic properties. The objective of this review is to summarize studies on diverse bioactive compounds and the beneficial properties of B. aegyptiaca.

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