ChemInform Abstract: INFLUENCE OF PHOSPHORYLATION ON THE PROPERTIES OF BIOLOGICALLY ACTIVE COMPOUNDS. I. PHOSPHORYLATED DERIVATIVES OF HYDROXYETHYLTHEOPHYLINE

1979 ◽  
Vol 10 (12) ◽  
Author(s):  
P. CHABRIER ◽  
N. T. THUONG ◽  
C. WAROLIN ◽  
O. FOUSSARD-BLANPIN ◽  
J. BRETAUDEAU ◽  
...  
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Derivatives Of

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

Chemical modification and Physicochemical properties of new derivatives 5-(thiophen-3-ilmethyl)-4-R1-1,2,4-triazole-3-thiol

2021 ◽  
pp. 4621-4629
Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
High Reactivity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Triazole Derivatives ◽  
Pharmaceutical Ingredients ◽  
Current Trends ◽  
Wide Range ◽  
Derivatives Of

Current trends in the search for new biologically active compounds among synthetic molecules have arguably proved a priority in studies of the heterocyclic 1,2,4-triazole system. For many years, 1,2,4-triazole derivatives remain the object of close attention of scientists of various scientific fields. The unique properties of 1,2,4-triazole derivatives include high reactivity, which allows different modification of this system, practical absence of toxicity of these derivatives and the presence of a wide range of biological, pharmacological properties, which in the complex provides the prerequisites for the creation of new biologically active compounds, and in the future, active pharmaceutical ingredients (AFI). The aim of our work is to investigate some transformations in a number of derivatives of 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiol, to study the physicochemical properties of the new synthesized compounds. A well-known fact remains the successful attempt of many scientists involved in the study of the heterocyclic 1,2,4-triazole system to synthesize potential biologically active compounds. The process of creating new molecules is very painstaking and requires considerable effort. The chemical approaches for the synthesis of the starting compounds required for further transformations are well known and described. Therefore, we used the corresponding N-R1-2 as intermediates for the synthesis of new 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiols appropriate ones were used N-R1-2-(2-(thiophen-3-yl) acetyl) hydrazinocarbothioamide.

Piperazine derivatives of boronic acids – potential bifunctional biologically active compounds

2015 ◽  
Vol 39 (6) ◽  
pp. 4308-4315 ◽  
Author(s):  
Agnieszka Adamczyk-Woźniak ◽  
Karolina Czerwińska ◽  
Izabela D. Madura ◽  
Alicja Matuszewska ◽  
Andrzej Sporzyński ◽  
...  
Keyword(s):  
Biological Activity ◽  
Boronic Acids ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Piperazine Derivatives ◽  
Derivatives Of

The combination of a piperazine and boronic groups within one molecule can result in a totally novel biological activity.

scholarly journals ДОСЛІДЖЕННЯ ГОСТРОЇ ТОКСИЧНОСТІ ПОХІДНИХ 1,2,4-ТРІАЗОЛУ, ЩО МІСТЯТЬ В СВОЄМУ СКЛАДІ ЯДРО 1Н-ТЕТРАЗОЛУ

2019 ◽  
pp. 23-30
Author(s):  
Фролова Ю. С. ◽  
Каплаушенко А. Г.
Keyword(s):  
Acute Toxicity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
New Drugs ◽  
Active Compounds ◽  
Multi Stage ◽  
Preclinical Trials ◽  
Stage Process ◽  
Derivatives Of

The design of new drugs is a rather complex and multi-stage process. The modeling and creation of new biologically active compounds are one of the stages of this operation. One of the important stages of preclinical trials is the study of acute toxicity of newly synthesized compounds. Great interest in this branch is nitrogen-containing heterocycles, namely 1,2,4-triazole and their derivatives.Therefore, the purpose of our work is to study acute toxicity among new derivatives of 5-(1H-tetrazole-1-yl)-4-R-3-thio(amino)-1,2,4-triazole. The study of acute toxicity was carried out by the method of V. B. Prozorovsky on the white nonlinear rats.As a result of the experiments, acute toxicity of the 41 synthesized compounds was determined. The value of the LD50 of new derivatives of 5-(1H-tetrazole-1-yl)-4-R-3-thio(amino)-1,2,4-triazole is in the range of 357-1060 mg/kg, and according to the classification of Sidorov I. K. belong to IV and V toxicity classes.

scholarly journals Analogs of biologically active compounds VIII. Synthesis of some derivatives of 6-azalumazine

ARKIVOC ◽  
2005 ◽  
Vol 2006 (1) ◽  
pp. 68-75
Author(s):  
Jakub Stýskala ◽  
Jan Slouka ◽  
Vlasta Švecová
Keyword(s):  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Derivatives Of
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