Diazocarbonyl derivatives of amino acids: unique chiral building blocks for the synthesis of biologically active compounds

2019 ◽  
Vol 88 (3) ◽  
pp. 248-279 ◽  
Author(s):  
D P Zarezin ◽  
V G Nenajdenko
Keyword(s):  
Amino Acids ◽  
Building Blocks ◽  
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.

scholarly journals Cyclic cis-1,3-Diamines Derived from Bicyclic Hydrazines: Synthesis and Applications

Synlett ◽  
2020 ◽  
Author(s):  
Erica Benedetti ◽  
Laurent Micouin ◽  
Claire Fleurisson
Keyword(s):  
Bond Cleavage ◽  
Building Blocks ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Chemical Similarity ◽  
Active Compounds ◽  
General Overview ◽  
Biological Interest ◽  
Potential Applications ◽  
Rna Binders

AbstractCyclic cis-1,3-diamines are versatile building blocks frequently found in natural molecules or biologically active compounds. In comparison with widely studied 1,2-diamines, and despite their chemical similarity, 1,3-diamines have been investigated less intensively probably because of a lack of general synthetic procedures giving access to these compounds with good levels of chemo-, regio-, and stereocontrol. In this Account we will give a general overview of the biological interest of cyclic cis-1,3-diamines. We will then describe the synthesis and potential applications of these compounds with a particular focus on the work realized in our laboratory.1 Introduction2 Biological Relevance of the cis-1,3-Diamine Motif3 Classical Synthetic Strategies towards cis-1,3-Diamines4 N–N Bond Cleavage of Bicyclic Hydrazines: A Versatile Method to Access cis-1,3-Diamines4.1 Preparation of Five-Membered Cyclic cis-1,3-Diamino Alcohols4.2 Access to Fluorinated 1,3-cis-Diaminocyclopentanes4.3 Synthesis of cis-1,3-Diaminocyclohexitols4.4 Formation of Cyclic cis-3,5-Diaminopiperidines5 Applications of Cyclic cis-1,3-Diamines5.1 Small-Molecular RNA Binders5.2 Fluorinated 1,3-Diamino Cyclopentanes as NMR Probes6 Concluding Remarks

ChemInform Abstract: Synthesis of New Racemic and Optically Active N-Phosphonoalkyl Bicyclic β-Amino Acids via the Kabachnik-Fields Reaction as Potential Biologically Active Compounds.

ChemInform ◽  
2012 ◽  
Vol 43 (30) ◽  
pp. no-no
Author(s):  
Petar T. Todorov ◽  
Nikola D. Pavlov ◽  
Boris L. Shivachev ◽  
Rosica N. Petrova ◽  
Jean Martinez ◽  
...  
Keyword(s):  
Amino Acids ◽  
Optically Active ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds

Electrochemical Regioselective C–H Selenylation of 2H-Indazole Derivatives

2021 ◽  
Author(s):  
Zhixiong Ruan ◽  
Shengsheng Lin ◽  
Xiaomei Cheng ◽  
Hasimujiang Balati ◽  
Zhongnan Xu ◽  
...  
Keyword(s):  
Environmentally Friendly ◽  
Building Blocks ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds

The selenium-substituted heteroarenes are biologically active compounds and useful building blocks. In this sequence, we have developed a metal-and oxidant-free, environmentally friendly protocol for the regioselective selenylation of 2H-indazole derivatives...

scholarly journals INFLUENCE OF BIOTECHNOLOGICAL FACTORS ON THE YIELD OF BIOLOGICALLY ACTIVE COMPOUNDS FROM SORBUS AUCUPARIA

2021 ◽  
pp. 291-300
Author(s):  
Elena Nikolaevna Sokolova ◽  
Tat'yana Vladimirovna Yuraskina ◽  
Yuliya Aleksandrovna Borshcheva ◽  
Natal'ya Aleksandrovna Fursova ◽  
Anton Yur'yevich Sharikov ◽  
...  
Keyword(s):  
Amino Acids ◽  
Biologically Active Compounds ◽  
Biologically Active Substances ◽  
Biologically Active ◽  
Theoretical Research ◽  
Sorbus Aucuparia ◽  
Plant Materials ◽  
Active Compounds ◽  
Wide Range ◽  
Active Substances

Currently, the diet of almost all population groups in Russia is characterized by a deficiency of vitamins, essential amino acids, macro- and micronutrients, as well as biologically active substances (flavonoids, carotenoids, etc.). Replenishment of the lack of these components in the diet of the population due to natural sources of plant origin is an important and actual task of national health care. The rational use of natural components of plant materials containing a wide range of natural biologically active substances using biocatalytic methods, as well as the selection of optimal conditions for obtaining commodity forms of ingredients, will allow to create preventive products that have a beneficial effect on the human body. Theoretical research in the field of promising sources of food and biologically active ingredients among wild species of plant materials were carried out. Biomedical properties of Sorbus aucuparia were described. The technological characteristics of the biologically active substances extraction from dried plant raw materials was investigated. Thus, it was revealed that the degree of dried berries grinding about 0.2–0.8 mm, the hydromodule 1 : 10 and the extraction duration 240 minutes are most effective for the extractive substances yield. The enzymatic complex, allowing the maximum to release biologically valuable components to extract was selected. The amino acid composition of rowanberry with the use of high-performance liquid chromatography was investigated. Produced fermentalizates contain complex of biologically active compounds, including amino acids, vitamins, carotenoids, phenolic substances, that makes these ingredients promising for creation of various foodstuffs to improve quality, nutritional and biological value, taste and other consumer properties.

Sign in / Sign up

Export Citation Format

Share Document