scholarly journals Pharmacological Profile of Quinoxalinone

2014 ◽  
Vol 2014 ◽  
pp. 1-21 ◽  
Author(s):  
Youssef Ramli ◽  
Ahmed Moussaif ◽  
Khalid Karrouchi ◽  
El Mokhtar Essassi
Keyword(s):  
Organic Synthesis ◽  
Active Compound ◽  
Antitubercular Activity ◽  
Biologically Active ◽  
Efficacy And Safety ◽  
Pharmacological Profile ◽  
Synthetic Compounds ◽  
Biologically Active Compound ◽  
Anti Inflammatory ◽  
Quinoxalinone Derivatives

Quinoxalinone and its derivatives are used in organic synthesis for building natural and designed synthetic compounds and they have been frequently utilized as suitable skeletons for the design of biologically active compound. This review covers updated information on the most active quinoxalinone derivatives that have been reported to show considerable pharmacological actions such as antimicrobial, anti-inflammatory, antidiabetic, antiviral, antitumor, and antitubercular activity. It can act as an important tool for chemists to develop newer quinoxalinone derivatives that may prove to be better agents in terms of efficacy and safety.

scholarly journals Design, Synthesis, Characterization, Computational Study and In-vitro Antioxidant and Anti-inflammatory Activities of Few Novel Pyrazol-3-one Derivatives

2021 ◽  
pp. 220-231
Author(s):  
Aziz Unnisa ◽  
B. Anupama ◽  
Humera Banu ◽  
Syeda B. Fatima ◽  
K. N. V. Chenchu Lakshmi ◽  
...  
Keyword(s):  
Computational Study ◽  
Efficacy And Safety ◽  
Dpph Assay ◽  
Design Synthesis ◽  
Synthetic Compounds ◽  
Highly Active ◽  
Anti Inflammatory ◽  
Further Development ◽  
Mutagenic Compound

Aim: To design, synthesize and perform computational study on a few Novel pyrazol-3-one derivatives. Study design:  Experimental study. Methodology: A series of 6-aryl substituted pyrimidine azodyes were synthesized by coupling phenyl pyrimidine 2-amine with different aromatic amines. The synthetic compounds were screened for their in-vitro antioxidant and anti-inflammatory activities. The Computational study of designed compounds was done by OCHEM, Molinspiration cheminformatics, Datawarrior, and Swiss ADME. DPPH assay was used to determine the antioxidant activity and heat hemolysis method for anti-inflammatory activity. Results: Molinspiration, Data Warrior, Ochem which are helpful to predict molecule general properties, bioactive scores, toxicity, and drug-likeness. Data Warrior results inferred that the compounds possess moderately active towards mutagenic (compound 2, 11), reproductive (compound 6, 7, 8), and highly active towards Tumorogenic (compound 2) toxicities. OCHEM results showed that most of the synthesized compounds were found to be non-inhibitors of all the subtypes of cytochrome P450 except compound 8. All compounds under this study were effective scavengers of free radicals except the compounds 1, 2, 6, 10. Invitro Anti-inflammatory studies have shown that the compounds (6, 7, 8, 9, 13) active toward heat hemolysis. Conclusion: The synthesized compounds were comprehensively studied and targets were identified rendering them as lead molecules for further development of newer agents with greater efficacy and safety.

scholarly journals Medical and biological functions of water

2019 ◽  
pp. 65-75
Author(s):  
R. S. Korytniuk ◽  
L. L. Davtian ◽  
N. I. Hudz ◽  
A. A. Drozdova ◽  
I. О. Vlasenko ◽  
...  
Keyword(s):  
Osmotic Pressure ◽  
Active Compound ◽  
The Body ◽  
Biologically Active ◽  
Biological Functions ◽  
Salt Balance ◽  
Biologically Active Compound ◽  
Water Salt ◽  
Excessive Intake ◽  
Pharmaceutical Practice

Water is the most common compound of hydrogen and oxygen in the nature. It is a universal solvent of many substances, and therefore chemically pure water does not exist in the nature. The water contained in the body is qualitatively different from ordinary water as it is structured water. Such crystalline structures of water are the matrix of life. Their presence gives possibility of the occurrence of important biophysical processes and biochemical reactions. Insufficient intake of water into the body or its excessive loss leads to dehydration, which is accompanied by thickening of the blood and impairing hemodynamics. Excessive intake of water into the body causes water intoxication. Purpose – to conduct a bibliosemantic analysis of the sources of the literature on the medical and biological functions of water. Research methods – bibliosemantic, analytical, logical methods and generalizion method. Water is the structural basis of cells necessary to maintain their optimal volume. It determines the spatial structure and function of biomolecules. Insufficient intake of water into the body or its excessive loss leads to an impaired hemodynamics. Excessive intake of water into the body causes water intoxication. All disoders of water-salt balance in the body can be divided into two groups: dehydration and hyperhydration. In each group, there are disorders with a decrease, increase, and no change in osmotic pressure (hypotonic, hypertonic, and isotonic disorders, respectively). Water is used in medical and pharmaceutical practice as an excipient, and for the manufacture of allopathic, homeopathic and anthroposophic medicines. The State Pharmacopoeia of Ukraine includes several articles on the use of water depending on the purpose and regulates water quality: 1) highly purified water, water for injections «in bulk» water and sterilised water for injections; 2) purified water: water «in bulk» and water in containers. Cosmetics are presented on the Ukrainian market, the main biologically active compound of which is water, in particular, natural, thermal and micellar. They are widely used in cosmetology. The biomedical function of water in the body is to preserve cell volume, provide turgor to the cells and save the body from temperature fluctuations. Disruption of water-salt balance leads to dehydration or hyperhydration. There are changes with a decrease, increase, and no change in osmotic pressure (hypotonic, hypertonic, and isotonic disorders, respectively). They cause disruption of the life of the whole organism. In pharmaceutical practice, water is widely used for the manufacture of allopathic, homeopathic and anthroposophic medicines. It can be obtained in various ways, but its quality is regulated by the relevant government regulations. In cosmetic practice, water is used not only as a basic solvent, but in the form of natural, micellar and thermal water, where it is a biologically active compound.

scholarly journals STUDY OF THE INFLUENCE OF 6-(40 -IODOPHENYL)-2,3-DIHYDRO [2,1-B] THIAZOLE AT THYROID FUNCTION MALE WHITE RATS WITH EXPERIMENTAL AUTOIMMUNE THYROIDITIS

2016 ◽  
Vol 57 (3) ◽  
pp. 43-49
Author(s):  
N. G. Malova ◽  
L. A. Sirotenko ◽  
I. V. Komarova ◽  
E. S. Anikeeva ◽  
A. V. Spiridonov ◽  
...  
Keyword(s):  
Thyroid Gland ◽  
T Lymphocytes ◽  
Thyroid Function ◽  
Autoimmune Thyroiditis ◽  
Active Compound ◽  
Biologically Active ◽  
Experimental Autoimmune Thyroiditis ◽  
White Rats ◽  
Biologically Active Compound ◽  
Experimental Autoimmune

The study of new biologically active compound PL-308 with immunomodulating properties on the thyroid function in rats with experimental autoimmune thyroiditis. It was determined that the introduction of PL-308 reduces autoimmune aggression by lowering the level of antibodies to thyroglobulin, increases the number of all subpopulations of T-lymphocytes, in particular Tsuppressors. It was observed normalization of the functional state of the thyroid gland.

scholarly journals Development and validation of methods of quantitative determination of biologically active compound n-(2-[4-oxo-3(4h)-quinazolinyl]propionyl)guanidine

2020 ◽  
Vol 19 (5-6) ◽  
pp. 122-127
Author(s):  
Evgenia V. Kompantseva ◽  
Daria N. Lutsenko ◽  
Alexander A. Glushko
Keyword(s):  
Quantitative Determination ◽  
Active Compound ◽  
Molecular Form ◽  
Biologically Active ◽  
Ionization Constants ◽  
Error Limit ◽  
Analytical Wavelength ◽  
Biologically Active Compound ◽  
Development And Validation

This paper presents the results of the selection and justification of the conditions for determination of a new biologically active compound (BAC) VMA-13-15, which is N-(2-[4-oxo-3(4H)-quinazolinyl]propionyl)guanidine bymeans of the spectrophotometry. By using the calculated values of BAC ionization constants, it was proposed to use purified water as a solvent. The maximum light absorption at 266 nm was chosen as the analytical wavelength. This was justified by the fact that in aqueous solutions 99% BAC are in the molecular form, which allows to determine it with the error limit of 1.29%, and with the least amount of dilutions. The study showed that the proposed method is specific and linear in the analytical concentration of 0.0010.004%, as well as it is precise and correct, which confirms the possibility of its use for quantitative determination.

scholarly journals Karalicin, a New Biologically Active Compound from Pseudomonas fluorescens/putida. II. Biological Properties.

1996 ◽  
Vol 49 (3) ◽  
pp. 263-266 ◽  
Author(s):  
GIORGIO LAMPIS ◽  
DELIA DEIDDA ◽  
CARLO MAULLU ◽  
SABRINA PETRUZZELLI ◽  
RAFFAELLO POMPEI ◽  
...  
Keyword(s):  
Pseudomonas Fluorescens ◽  
Active Compound ◽  
Biological Properties ◽  
Biologically Active ◽  
Biologically Active Compound

scholarly journals Hepatocytes produce nitrogen oxides from L-arginine in response to inflammatory products of Kupffer cells.

1989 ◽  
Vol 170 (5) ◽  
pp. 1769-1774 ◽  
Author(s):  
R D Curran ◽  
T R Billiar ◽  
D J Stuehr ◽  
K Hofmann ◽  
R L Simmons
Keyword(s):  
Endothelial Cells ◽  
Protein Synthesis ◽  
Nitrogen Oxides ◽  
Kupffer Cells ◽  
Metabolic Pathway ◽  
Active Compound ◽  
Total Protein ◽  
Biologically Active ◽  
Biologically Active Compound

A metabolic pathway by which L-arginine (L-arg) is converted to the biologically active compound NO. has recently been described in macrophages (M phi) and endothelial cells. This report demonstrates that transferable products from activated Kupffer cells (KC) induce the conversion of large quantities of L-arg to nitrogen oxides within hepatocytes (HC). In M phi and endothelial cells, citrulline and NO2-/NO3- are the stable endproducts of this metabolic pathway. In contrast, HC L-arg metabolism resulted in significantly greater production of NO2-/NO3- than citrulline. The generation of NO. within HC was associated with a concurrent decrease in total protein synthesis.

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