Synthesis, physical-chemical properties and the study of anti-hypoxemic activity of 5-(adamantane-1-yl)-4-R-1,2,4-triazole-3-thion alkylderivatives

Odyntsova, V. M.; Pruglo, Ye. S.

doi:10.14739/2310-1210.2015.2.42123

Cited by 2 publications

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“…In the mass spectrum, there are molecular ion peaks and fragment ion peaks that confirm this structure. 3,thiadiazole-2-ylthio) methyl) -1,2,4-triazole-3-thione (2.1). 1 H NMR (400 MHz), δ, ppm: 9.76 (s, 1H, NH), 7.62-7.59 (m, 2H, C 6 H 5 NH), 1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione were presented in this work.…”

Section: Resultsmentioning

confidence: 99%

“…На наступних етапах досліджень планується встановлення показників антимікробної активності синтезованих речовин. The prospect of pharmaceutical research remains the search for biologically active substances among molecules that combine heterocyclic moieties of different nature [1][2][3][4][5][7][8][9]. Examples of such fragments are 1,2,4-triazole and thiadiazole, which have significant synthetic and pharmacological potential [6].…”

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Synthesis and properties of some S-derivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione

Gotsulya

Fedotov

2019

Current Issues in Pharmacy and Medicine: Science and Practice

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A -research concept and design; B -collection and/or assembly of data; C -data analysis and interpretation; D -writing the article; E -critical revision of the article; F -final approval of the article Studies in the field of chemistry and pharmacology of derivatives of thiadiazole and 1,2,4-triazole are promising and relevant, which is associated with significant success in creating new drugs based on them. The combination of these heterocycles in one molecule makes it possible to increase the probability of detecting substances with a certain type of biological activity among the synthesized compounds.The aim of the work was to optimize the synthesis and study of the properties of S-alkyl derivatives of 5-R-4-phenyl-1,2,4-triazole-3thione, containing a thiadiazole fragment in their structure, as well as the prediction of possible biological activity to rating the prospects of further studies in vivo and in vitro. Materials and methods.As a key starting reagent, 3-amino-1-phenylthiourea was used. Using the reaction between the starting reagent and carbon disulfide in DMF, thion was obtained, which was further alkylated with isopropyl chloroacetate. The resulting reaction product was then used for subsequent transformations using hydrazinolysis reactions, nucleophilic addition of phenylisothiocyanate and intramolecular alkaline heterocyclization. A number of S-derivatives of the obtained 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione were synthesized by the interaction with haloalkanes in the presence of an equivalent amount of alkali in alcoholic medium. The structure of the obtained compounds was confirmed by elemental analysis, 1 H NMR spectroscopy, and IR-spectrophotometry. The individuality of substances was established by high performance liquid chromatography. For the synthesized substances, an individual calculated screening was performed using the PASS Online ® software product.Results. The procedure for preparing 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione was optimized. The optimal synthesis conditions were determined S-alkylderivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thiol, the structure was established the obtained substances and their physical properties were studied. With the help of computer-assisted prediction Pass Online ® , a promising direction for further studies of the biological activity of the target reaction products was determined. Conclusions.A series of S-alkylderivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione were obtained, the structure of these compounds was confirmed by physical-chemical methods of analysis. At the next stages of the study, it would be planned to establish indicators of the antimicrobial activity of the synthesized substances. Синтез і властивості деяких S-похідних 4-феніл-5-((5-феніламіно-1,3,4-тіадіазол-2-ілтіо)метил)-1,2,4-тріазол-3-тіону C. O. Федотов, А. С. ГоцуляДослідження в галуз...

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Section: Resultsmentioning

confidence: 99%

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Synthesis and properties of some S-derivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione

Gotsulya

Fedotov

2019

Current Issues in Pharmacy and Medicine: Science and Practice

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“…Separately to the ability to proliferate, 1,2,4-triazole derivatives are able to have a cytoprotective effect. Cytoprotection is manifested in antioxidant [41][42][43][44][45], antihypoxic [46][47][48][49][50], hepatoprotective [51][52][53][54][55], neuroprotective [56][57][58][59][60] action. In particular, scientists [60] conducted an extensive review of 64 compounds that can find their application in the treatment of Alzheimer's disease.…”

Section: Cytoprotective Activity Of 124-triazolesmentioning

confidence: 99%

“…7). In the analyzed works [41][42][43][44][45][46][47][48][49][50][51][52][53][54][55][56][57][58][59][60], 40 potential antioxidants were identified, among which the authors separately Note 4 molecules; 44 compounds with antihypoxic activity were identified, of which 5 are recommended for further study. 106 potential neuroprotectors were identified, of which 7 attract special attention of scientists.…”

Section: Cytoprotective Activity Of 124-triazolesmentioning

confidence: 99%

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

et al. 2022

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The authors are not native speakers of Turkish The purpose of this literature review was to systematize data from studies of the biological activity of 1,2,4-triazole derivatives with substituents in positions 4 and 5. The authors set the task of forming an idea of current directions in the selection of substitutions for 1,2,4-triazole based on research. As a result of the study, 75 literature sources were analyzed. This made it possible to form a further vector in terms of searching for biologically active structures among 1,2,4-triazole derivatives. The review develops a modern approach to the search for biologically active substances among 1,2,4-triazole derivatives. Systematized data on the nature of substituents in the core of 1,2,4-triazole, which affect a specific type of activity. The search material was selected over the past decade with the highest number of citations at the time of literature analysis.

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Synthesis, physical-chemical properties and the study of anti-hypoxemic activity of 5-(adamantane-1-yl)-4-R-1,2,4-triazole-3-thion alkylderivatives

Cited by 2 publications

References 0 publications

Synthesis and properties of some S-derivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione

Synthesis and properties of some S-derivatives of 4-phenyl-5-((5-phenylamino-1,3,4-thiadiazole-2-ylthio)methyl)-1,2,4-triazole-3-thione

Prospects for the search for new biologically active compounds among the derivatives of the heterocyclic system of 1,2,4-triazole.

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