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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Format: | Article |
Language: | English |
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Zaporozhye State Medical University
2015-12-01
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Series: | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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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. |
first_indexed | 2024-04-12T16:01:06Z |
format | Article |
id | doaj.art-1773f53f946a4ac1af831f80c9175cf6 |
institution | Directory Open Access Journal |
issn | 2306-8094 2409-2932 |
language | English |
last_indexed | 2024-04-12T16:01:06Z |
publishDate | 2015-12-01 |
publisher | Zaporozhye State Medical University |
record_format | Article |
series | Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki |
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 |
work_keys_str_mv | AT dgivanchenko synthesisphysicalchemicalandbiologicalpropertiesof18disubstitutedoftheobromineív8rthioderivativesof1pmethylbenzyltheobronine |