The physicochemical basis of the biological activity and pharmacological properties of the antiviral agent Panavir

2014 ◽  
Vol 69 (6) ◽  
pp. 542-547 ◽  
Author(s):  
S. V. Stovbun ◽  
L. V. Yakovenko
Keyword(s):  
Biological Activity ◽  
Antiviral Agent ◽  
Pharmacological Properties ◽  
Physicochemical Basis

scholarly journals Isolation, Structure Elucidation, and Biological Activity of a New Alkaloid from Zanthoxylum rhetsa

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601
Author(s):  
Karsten Krohn ◽  
Stephan Cludius-Brandt ◽  
Barbara Schulz ◽  
Mambatta Sreelekha ◽  
Pottachola Mohamed Shafi
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Medicinal Plant ◽  
Plant Extract ◽  
Structure Elucidation ◽  
Biologically Active ◽  
Reduction Product ◽  
Pharmacological Properties ◽  
Evergreen Tree

Several biologically active alkaloids (1-4, 6), including a new quinazoline-6-carboxylic acid (1), were isolated from the medicinal plant Zanthoxylum rhetsa, an evergreen tree, native to subtropical areas. Whereas the pharmacological properties of the plant extract and single constituents have been widely tested, we now show that all of the metabolites have antialgal activities, all but 6 are antibacterial, and 6 and the reduction product 5 (derived from 4) are also antifungal.

scholarly journals Essentials Oils from Brazilian Eugenia and Syzygium Species and Their Biological Activities

Biomolecules ◽  
2020 ◽  
Vol 10 (8) ◽  
pp. 1155
Author(s):  
Jamile S. da Costa ◽  
Ellen de Nazaré S. da Cruz ◽  
William N. Setzer ◽  
Joyce Kelly do R. da Silva ◽  
José Guilherme S. Maia ◽  
...  
Keyword(s):  
Biological Activity ◽  
South America ◽  
Biological Activities ◽  
Herbal Medicines ◽  
Chemical Diversity ◽  
Pharmacological Properties ◽  
Sesquiterpene Hydrocarbons ◽  
Leishmania Spp ◽  
Alternative Sources ◽  
Interspecific Diversity

The Eugenia and Syzygium genera include approximately 1000 and 1800 species, respectively, and both belong to the Myrtaceae. Their species present economic and medicinal importance and pharmacological properties. Due to their chemical diversity and biological activity, we are reporting the essential oils of 48 species of these two genera, which grow in South America and found mainly in Brazil. Chemically, a total of 127 oil samples have been described and displayed a higher intraspecific and interspecific diversity for both Eugenia spp. and Syzygium spp., according to the site of collection or seasonality. The main volatile compounds were sesquiterpene hydrocarbons and oxygenated sesquiterpenes, mainly with caryophyllane and germacrane skeletons and monoterpenes of mostly the pinane type. The oils presented many biological activities, especially antimicrobial (antifungal and antibacterial), anticholinesterase, anticancer (breast, gastric, melanoma, prostate), antiprotozoal (Leishmania spp.), antioxidant, acaricidal, antinociceptive and anti-inflammatory. These studies can contribute to the rational and economic exploration of Eugenia and Syzygium species once they have been identified as potent natural and alternative sources to the production of new herbal medicines.

scholarly journals Design and Synthesis of a Highly Simplified Pateamine Analogue

2021 ◽  
Author(s):  
◽  
Sarah Brown
Keyword(s):  
Biological Activity ◽  
Antiviral Agent ◽  
Triazole Ring ◽  
Initiation Factor ◽  
Thiazole Ring ◽  
Coupling Reactions ◽  
Design And Synthesis ◽  
Anticancer Properties ◽  
Bioactivity Assay ◽  
Mycale Hentscheli

<p>Pateamine (1) is a natural product from the marine sponge Mycale hentscheli that exhibits potent anticancer properties, and has potential as an antiviral agent, and in preventing the muscle wasting disorder cachexia. This biological activity of pateamine is due to its ability to inhibit the eukaryotic initiation factor eIF4A, which leads to the formation of stress granules, the inhibition of protein synthesis, and ultimately cell death. Unfortunately, pateamine is obtained in very small amounts from Mycale hentscheli; thus, it is necessary to synthesise pateamine and novel structural analogues in the laboratory. Previously a separate binding and scaffolding domain of pateamine was proposed, which led to the synthesis of a simplified des-methyl des- amino analogue that reduced the number of synthetic steps compared to pateamine while retaining its biological activity. This was followed by the synthesis of a simplified triazole- containing analogue 9 6 ; unfortunately, this exhibited substantially reduced bioactivity compared to pateamine, and it is therefore necessary to determine if the reduction in bioactivity was due to the replacement of the thiazole ring with a triazole ring, or due to the removal of key methyl groups of pateamine. Thus, the thiazole-containing analogue of 96 is deemed to be an important synthetic target.  In this Master’s project a highly simplified side chain-free analogue 130 was synthesised, which laid the groundwork for future synthesis of a thiazole-containing analogue of 96. The synthesis of 130 was achieved through a convergent synthesis with one commercially available and two prepared fragments. Particular attention was paid to the development of an efficient thiazole formation methodology, as well as optimising fragment synthesis and coupling reactions. Determination of the binding of analogue 130 with eIF4A using a competitive bioactivity assay in the presence of pateamine was then undertaken, which showed that either 130 does not bind to eIF4A or that it binds non-covalently and is then displaced by pateamine.</p>

scholarly journals Design and Synthesis of a Highly Simplified Pateamine Analogue

2021 ◽  
Author(s):  
◽  
Sarah Brown
Keyword(s):  
Biological Activity ◽  
Antiviral Agent ◽  
Triazole Ring ◽  
Initiation Factor ◽  
Thiazole Ring ◽  
Coupling Reactions ◽  
Design And Synthesis ◽  
Anticancer Properties ◽  
Bioactivity Assay ◽  
Mycale Hentscheli

<p>Pateamine (1) is a natural product from the marine sponge Mycale hentscheli that exhibits potent anticancer properties, and has potential as an antiviral agent, and in preventing the muscle wasting disorder cachexia. This biological activity of pateamine is due to its ability to inhibit the eukaryotic initiation factor eIF4A, which leads to the formation of stress granules, the inhibition of protein synthesis, and ultimately cell death. Unfortunately, pateamine is obtained in very small amounts from Mycale hentscheli; thus, it is necessary to synthesise pateamine and novel structural analogues in the laboratory. Previously a separate binding and scaffolding domain of pateamine was proposed, which led to the synthesis of a simplified des-methyl des- amino analogue that reduced the number of synthetic steps compared to pateamine while retaining its biological activity. This was followed by the synthesis of a simplified triazole- containing analogue 9 6 ; unfortunately, this exhibited substantially reduced bioactivity compared to pateamine, and it is therefore necessary to determine if the reduction in bioactivity was due to the replacement of the thiazole ring with a triazole ring, or due to the removal of key methyl groups of pateamine. Thus, the thiazole-containing analogue of 96 is deemed to be an important synthetic target.  In this Master’s project a highly simplified side chain-free analogue 130 was synthesised, which laid the groundwork for future synthesis of a thiazole-containing analogue of 96. The synthesis of 130 was achieved through a convergent synthesis with one commercially available and two prepared fragments. Particular attention was paid to the development of an efficient thiazole formation methodology, as well as optimising fragment synthesis and coupling reactions. Determination of the binding of analogue 130 with eIF4A using a competitive bioactivity assay in the presence of pateamine was then undertaken, which showed that either 130 does not bind to eIF4A or that it binds non-covalently and is then displaced by pateamine.</p>

scholarly journals Synthesis and Anti-HIV Activity of Carbamates of Antiviral Agent Stavudine

2002 ◽  
Vol 13 (5) ◽  
pp. 289-297
Author(s):  
TK Venkatachalam ◽  
P Samuel ◽  
IV Kourinov ◽  
FM Uckun
Keyword(s):  
Biological Activity ◽  
Antiviral Agent ◽  
Heterocyclic Amines ◽  
Efficient Synthesis ◽  
Hiv Replication ◽  
Derivatives Of ◽  
Anti Hiv

An efficient synthesis of carbamate analogues of the NRTI compound stavudine, has been achieved in five steps starting from commercially available thymidine. The synthesis involves conversion of thymidine into stavudine followed by condensation with carbaimidazole derivative obtained from various aromatic and heterocyclic amines in dimethylformamide solvent. The analogues thus obtained were further purified by crystallization to furnish analytically pure products. Examination of biological activity of these carbamate derivatives of stavudine showed that they inhibited HIV replication only at micro-molar concentrations.

New biological activity against phospholipase A2 by Turmerin, a protein from Curcuma longa L.

2008 ◽  
Vol 389 (3) ◽  
pp. 299-303 ◽  
Author(s):  
Mukunda Chethankumar ◽  
Leela Srinivas
Keyword(s):  
Biological Activity ◽  
Enzymatic Activity ◽  
Molecular Mass ◽  
Mixed Type ◽  
Curcuma Longa ◽  
Molar Ratio ◽  
Relative Molecular Mass ◽  
Pharmacological Properties ◽  
Naja Naja ◽  
Burk Plot

Abstract Turmerin is a protein from Turmeric (Curcuma longa L.) with a relative molecular mass of 14 kDa. The protein inhibits the enzymatic activity and neutralises the pharmacological properties, such as cytotoxicity, oedema and myotoxicity of multitoxic phospholipase A2 (NV-PLA2) of cobra (Naja naja) venom at a 1:2.5 molar ratio of NV-PLA2:Turmerin. A Lineweaver-Burk plot indicates that Turmerin follows a linear mixed type of inhibition.

scholarly journals Biological activity of heterocyclic systems based on functionally substituted 1,3,4-thia(oxa)diazoles (a review)

2019 ◽  
pp. 43-53
Author(s):  
M. I. Lelyukh
Keyword(s):  
Hydrogen Bonding ◽  
Biological Activity ◽  
Antiviral Activity ◽  
Synergistic Effect ◽  
Pharmacological Activity ◽  
Medicinal Chemistry ◽  
Pharmacological Properties ◽  
Hydrogen Bonding Interactions ◽  
Wide Possibility ◽  
Pharmacological Potential

1,3,4-Thiadiazole and oxadiazole hetetocycles are well-known pharmacophore scaffolds, which possess wide possibility for chemical modification and identified diverse pharmacological potential. Such essential and many-sided activities let to consider the mentioned heterocycles as ones of the crucial for expression of pharmacological activity, which confirm their importance for medicinal chemistry. Moreover, 1,3,4-oxadiazole cycle is a bioisostere for carboxylic, amide and ester groups, which mostly contribute to enhancement the pharmacological activity by participating in hydrogen bonding interactions with different enzymes and receptors. The aim of the work was analysis of literature data about biological activity of non-condensed heterocyclic systems based on 1,3,4-thia(oxa)diazole rings as promising objects for modern bioorganic and medicinal chemistry. In this study are presented the analysis of actual literature data about pharmacological activity of heterocyclic systems based on 1,3,4-thiadiazole. It has been established that mentioned scaffolds were identified as the main structural component of biological agents with antimicrobial, anti-inflammatory, analgetic, antitumor antitubercular and antiviral activity. Moreover, the combination of 1,3,4-thiadiazole or 1,3,4-oxadiazole core with various heterocycles led to synergistic effect in many cases. Thus, mentioned scaffolds are important heterocyclic fragments that are considered as promising structural matrices for the construction of new drug-likes molecules. An analysis of the biological activity of 1,3,4-thia(oxa)diazole derivatives was carried out, which allowed to confirm their versatile pharmacological potential. Obtained data can be considered as background for further in-depth studies of chemical and pharmacological properties such heterocyclic systems with possible application in medicine.

"Synthesis, Identification and Assess the Biological and Laser Efficacy of New Compounds of Azetidine Derived from Benzidine "

2020 ◽  
Vol 7 (2) ◽  
pp. 12-25
Author(s):  
Adil Hussein Dalaf ◽  
Fawzi Hameed Jumaa
Keyword(s):  
Biological Activity ◽  
Organic Compounds ◽  
Heterocyclic Compounds ◽  
Spectroscopic Methods ◽  
Pharmacological Properties ◽  
High Biological Activity ◽  
Physical Measurements ◽  
New Compounds

"Preparation of heterocyclic compounds with new pharmacological properties. Preparation of organic compounds with high biological activity against bacterial germs. Diagnosis of prepared compounds by physical and spectroscopic methods. Spectroscopic and physical measurements validated the prepared compounds. Studying the effect of lasers on these compounds, as it has been proven that the rays do not affect them.

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