Particular Activity of Naphthacene Derivatives as Inducers of Zoxazolamine Hydroxylase Synthesis in Rats

1967 ◽  
Vol 22 (5) ◽  
pp. 532-534 ◽  
Author(s):  
N. P. Buu-Ηοϊ ◽  
Do-Phuoc Hien
Keyword(s):  
Biological Activity ◽  
High Activity ◽  
Chemical Structure ◽  
Structural Analogues ◽  
Derivatives Of

High activity as inducers of microsomal zoxazolamine hydroxylase synthesis in rats has been found to be remarkably frequent in derivatives of the linear tetracyclic hydrocarbon naphthacene and their heterocyclic structural analogues. The relationships between chemical structure and this type of biological activity, which is shown to be independent of carcinogenic properties, are discussed.

Chemical structure and biological activity ofo-disubstituted derivatives of benzene

1967 ◽  
Vol 23 (12) ◽  
pp. 1038-1038 ◽  
Author(s):  
K. Boček ◽  
J. Kopecký ◽  
M. Krivucová
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Derivatives Of

scholarly journals Analysis of the relationship between the predicted biological activity and the chemical structure of S-derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols

2021 ◽  
Vol 14 (2) ◽  
pp. 167-172
Author(s):  
O. A. Bigdan
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Plant Protection ◽  
Hypoxia Inducible Factor ◽  
Polymeric Materials ◽  
Plant Protection Products ◽  
New Drugs ◽  
Antihypoxic Activity ◽  
Oxidation Reactions ◽  
Derivatives Of

1,2,4-Triazole derivatives are actively used as components in the development of new drugs, plant protection products, polymeric materials, anti-corrosion agents and etc. Chemical modeling of substituted 1,2,4-triazoles due to the introduction of different pharmacophores into the structure is very popular among scientists in various fields. Today it is known that some S-derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols have antimicrobial activity. The aim of the work is to analyze the relationships between the predicted biological activity and the chemical structure of S-derivatives of 5-(5-bromofuran-2-yl) -4R-1,2,4-triazole-3-thiols. Materials and methods. Virtual screening of compounds was performed using the computer program PASS (Prediction of activity spectra for substances). The results of the forecast were issued in the form of a list of names of probable types of activity with estimates of the probabilities of presence (Pa) and absence of each activity (Pi), which had values from 0 to 1. Results. Analyzing the prediction of biological activity on protein targets from the group of enzymes, we can said that derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols were active in the group of oxyreductases (Glutathione reductase, mitochondrial; Cyclooxygenase-2; Hypoxia-inducible factor prolyl hydroxylase 2), which catalyzed oxidation reactions, the transfer of electrons from one molecule (reducer, electron donor) to another (oxidant, electron acceptor). These compounds can demonstrate antioxidant, antihypoxic activity. Conclusions. The conducted forecast of biological activity revealed that derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols are the most active and there is a probability to show antitumor, antiviral, antibacterial, diuretic, actoprotective, and antioxidant activity.

scholarly journals Synthesis and Antimicrobial Studies of New [Tetrakis (1, 2, 4-Triazole / 1, 3, 4-Oxadiazole / 1, 3, 4-Thiadiazole] [Bis-(Benzene-1, 3, 5-Triyl)] Dioxymethylene Compounds

2020 ◽  
pp. 234-245
Author(s):  
Ahmed Neamah Ayyash
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Chemical Structure ◽  
Acid Hydrazide ◽  
Basic Medium ◽  
Tosyl Chloride ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Concentrated Sulfuric Acid ◽  
Derivatives Of

     Synthesis of new heterocyclic compounds containing four five-membered rings together was the main goal of this work. The new derivatives of [tetrakis (1,2,4-triazole /1,3,4-thiadiazole /1,3,4-oxadiazole][bis-(benzene-1,3,5-triyl)] dioxymethylene A7-A18 were synthesized by the reaction of [bis-(dimethyl 5-yl-isophthalate)] dioxymethylene compound A1 which was previously prepared from the reaction of 1,2-dibromomethan and dimethyl 5-hydroxyisophthalate, then treated with hydrazine hydrate to yield the corresponding acid hydrazide A2. In the next step, compound A2 was refluxed with 4-substituted isothiocyanate to give substituted thiosemicarbazides A3-A6. The treatment of the latter compounds in basic medium of 2M of NaOH afforded 1,2,4-Triazole derivatives A7-A10. Whereas the reaction of the same compounds with concentrated sulfuric acid gave 1,3,4-thiadiazoles  A11-A14. Furthermore, the new derivatives of 1,3,4-oxadiazole A15-A18 were obtained by the reaction of thiosemicarbazides and tosyl chloride in presence of pyridine. (C. H. N.) elemental analysis, FT-IR, and 1HNMR techniques were used to characterize the chemical structure of some of the new synthesized compounds which also exhibited an important biological activity.

Chemical structure and biological activity ofp-disubstituted derivatives of benzene

1964 ◽  
Vol 20 (12) ◽  
pp. 667-668 ◽  
Author(s):  
K. Boček ◽  
J. Kopecký ◽  
M. Krivucová ◽  
D. Vlachová
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Derivatives Of

scholarly journals Chemical Structure and Biological Activity on m-and p-Disubstituted Derivatives of Benzene

Nature ◽  
1965 ◽  
Vol 207 (5000) ◽  
pp. 981-981 ◽  
Author(s):  
J. KOPECKÝ ◽  
K. BOČEK ◽  
D. VLACHOVÁ
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Derivatives Of

Structure-Dependent Biological Activity of Racemic 1-Substituted 2-0-Hexadecylglycero-3-phosphocholines and Analogues

1984 ◽  
Vol 39 (3-4) ◽  
pp. 252-256 ◽  
Author(s):  
Siegfried Kluge ◽  
Heinz-Peter Kertscher ◽  
Gunter Ostermann
Keyword(s):  
Biological Activity ◽  
High Activity ◽  
Glyceryl Ether ◽  
Potato Virus X ◽  
Acetyl Derivative ◽  
Methyl Derivative ◽  
Structural Element ◽  
Tobacco Plants ◽  
Test Systems ◽  
Structural Analogues

1-substituted 2-O-hexadecylglycero-3-phosphocholines and some structural analogues were tested for their biological activity on two entirely different test systems: human thrombocytes and potato virus X in tobacco plants. Structural prerequisites for a high activity in both systems are the alkyl glyceryl ether structural element, a short-chain substituent in the C-1 position, and the phosphocholine grouping. Accordingly, 1-O-methyl derivative (2) and 1-O-acetyl derivative (5) have the strongest effect on the biological activity of both test systems. The intensity of the effect of the tested compounds does not correlate with membranolytic properties measured by the lytic action on red cells

scholarly journals Synthesis of new 3-(2-aminothiazol-4-yl)-4-hydroxy-2H-chromen-2-one derivatives

2006 ◽  
Vol 71 (6) ◽  
pp. 581-585 ◽  
Author(s):  
S. Sukdolak ◽  
N. Vukovic ◽  
S. Solujic ◽  
M. Milosev ◽  
N. Manojlovic ◽  
...  
Keyword(s):  
Biological Activity ◽  
Nmr Spectroscopy ◽  
Structural Analysis ◽  
1H Nmr ◽  
1H Nmr Spectroscopy ◽  
Chemical Structure ◽  
High Yield ◽  
Thiourea Derivatives ◽  
Starting Compound ◽  
Derivatives Of

Aminothiazole derivatives of 4-hydroxy-2H-chromen-2-one were prepared by the Hantzsch reaction1 using 3-(2-bromoacetyl)-4-hydroxy-2H-chromen-2-one and thiourea derivatives. Starting compound for this synthesis 3-(2-bromoacetyl)-4-hydroxy- 2H-chromen-2-one (1) was prepared previously.2 Also, for this synthesis we used thiourea derivatives (2a-j) as compounds which possess groups with biological activity. Reactions are carried out in refluxing ethanol for a period of 30 - 45 min. Final products (3a-j) are obtained in a high yield. Chemical structure of the obtained compounds was confirmed by elemental and structural analysis (IR and 1H NMR spectroscopy).

scholarly journals Derivatives of 1,2,4-Triazole-3,4-Disubstituted Based on Aminoacids with Potential Biological Activity

2020 ◽  
Vol 71 (5) ◽  
pp. 211-221
Author(s):  
Corina Cheptea ◽  
Valeriu Sunel ◽  
Cezarina Morosanu ◽  
Dana Ortansa Dorohoi
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Malignant Tumors ◽  
Potential Biological Activity ◽  
New Compounds ◽  
Derivatives Of

In order to obtain new substances with potential biological activity dipeptide derivatives from p-aminobenzoyl-phenylglycine and p-aminobenzoyl-phenylalanine were grafted on 1,2,4-triazolic heterocycle. The new synthesized compounds belong to the group of antimetabolites, group used in medicine for treating malignant tumors. Also, it is possible to study the correlation between chemical structure and biological activity of the new compounds.

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