Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine

The problem of biologically active compounds searching amidst xanthine derivatives is a crucial one and is an issue for long-term investigation. Aim. In order to search for new biologically active compounds among xanthine derivatives, 8-R-thioderivatives of 1-p-methylbenzyltheobronine, undescribe...

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Main Author: D. G. Ivanchenko
Format: Article
Language:English
Published: Zaporozhye State Medical University 2015-12-01
Series:Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki
Subjects:
Online Access:http://pharmed.zsmu.edu.ua/article/view/52389/49765
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author D. G. Ivanchenko
author_facet D. G. Ivanchenko
author_sort D. G. Ivanchenko
collection DOAJ
description The problem of biologically active compounds searching amidst xanthine derivatives is a crucial one and is an issue for long-term investigation. Aim. In order to search for new biologically active compounds among xanthine derivatives, 8-R-thioderivatives of 1-p-methylbenzyltheobronine, undescribed earlier have been synthesized. Methods and results. Heating of 1-p-methylbenzyl-8-thiotheobromine with 2-bromo-4’-chloroacetophenone in aqueous ethanol leads to the formation of 1-p-methylbenzyl-8-[2-(4-chlorophenyl)-2-oxoethyl]thiotheobromine. Interaction of 8-thiotheobromine with chloroacetic acid methyl ester has lead to formation of (1-p-methylbenzyltheobromine-8-yl)thioacetic acid methyl ester. Structure of synthesized compounds has been definitely proved by NMR-spectroscopy. The acute toxicity, diuretic and antimicrobial activities of the obtained compounds have been explored. Conclusion. Priorities for further search of biologically active compounds in a range of xanthine derivatives have been set out.
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spelling doaj.art-1773f53f946a4ac1af831f80c9175cf62022-12-22T03:26:11ZengZaporozhye State Medical UniversityAktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki2306-80942409-29322015-12-0134810.14739/2409-2932.2015.3.52389Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronineD. G. IvanchenkoThe problem of biologically active compounds searching amidst xanthine derivatives is a crucial one and is an issue for long-term investigation. Aim. In order to search for new biologically active compounds among xanthine derivatives, 8-R-thioderivatives of 1-p-methylbenzyltheobronine, undescribed earlier have been synthesized. Methods and results. Heating of 1-p-methylbenzyl-8-thiotheobromine with 2-bromo-4’-chloroacetophenone in aqueous ethanol leads to the formation of 1-p-methylbenzyl-8-[2-(4-chlorophenyl)-2-oxoethyl]thiotheobromine. Interaction of 8-thiotheobromine with chloroacetic acid methyl ester has lead to formation of (1-p-methylbenzyltheobromine-8-yl)thioacetic acid methyl ester. Structure of synthesized compounds has been definitely proved by NMR-spectroscopy. The acute toxicity, diuretic and antimicrobial activities of the obtained compounds have been explored. Conclusion. Priorities for further search of biologically active compounds in a range of xanthine derivatives have been set out.http://pharmed.zsmu.edu.ua/article/view/52389/49765XanthineOrganic SynthesisNMR SpectroscopyAcute Toxicit TestsDiureticsAntibacterialAntifungal Agents
spellingShingle D. G. Ivanchenko
Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki
Xanthine
Organic Synthesis
NMR Spectroscopy
Acute Toxicit Tests
Diuretics
Antibacterial
Antifungal Agents
title Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
title_full Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
title_fullStr Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
title_full_unstemmed Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
title_short Synthesis, physical-chemical and biological properties of 1,8-disubstituted of theobromine. ІV. 8-R-thioderivatives of 1-p-methylbenzyltheobronine
title_sort synthesis physical chemical and biological properties of 1 8 disubstituted of theobromine іv 8 r thioderivatives of 1 p methylbenzyltheobronine
topic Xanthine
Organic Synthesis
NMR Spectroscopy
Acute Toxicit Tests
Diuretics
Antibacterial
Antifungal Agents
url http://pharmed.zsmu.edu.ua/article/view/52389/49765
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