Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes

Methods for the synthesis of hybrid molecules that combine the structure of a highly active antimicrobial compounds - tris(1-alkylindol-3-yl)methylium as well as 3-(indol-1-yl)maleimides that previously showed activity against some protein kinases have been developed. The main purpose of this study...

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Main Authors: S. N. Lavrenov, A. Yu. Simonov, A. A. Panov, S. A. Lakatosh, E. B. Isakova, E. A. Tsvigun, O. P. Bychkova, V. V. Tatarskiy, E. S. Ivanova, E. P. Mirchink, A. M. Korolev, A. S'. Trenin
Format: Article
Language:Russian
Published: LLC "Publishing House OKI" 2020-05-01
Series:Антибиотики и Химиотерапия
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Online Access:https://www.antibiotics-chemotherapy.ru/jour/article/view/89
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author S. N. Lavrenov
A. Yu. Simonov
A. A. Panov
S. A. Lakatosh
E. B. Isakova
E. A. Tsvigun
O. P. Bychkova
V. V. Tatarskiy
E. S. Ivanova
E. P. Mirchink
A. M. Korolev
A. S'. Trenin
author_facet S. N. Lavrenov
A. Yu. Simonov
A. A. Panov
S. A. Lakatosh
E. B. Isakova
E. A. Tsvigun
O. P. Bychkova
V. V. Tatarskiy
E. S. Ivanova
E. P. Mirchink
A. M. Korolev
A. S'. Trenin
author_sort S. N. Lavrenov
collection DOAJ
description Methods for the synthesis of hybrid molecules that combine the structure of a highly active antimicrobial compounds - tris(1-alkylindol-3-yl)methylium as well as 3-(indol-1-yl)maleimides that previously showed activity against some protein kinases have been developed. The main purpose of this study was to investigate the influence of substituents on the activity of compounds against different test microorganisms, as well as their toxicity on human cells. For example, with the introduction of a fragment of maleimide, it was possible to reduce cytotoxicity by almost 40 times compared to the original prototype in some cases. At the same time, antimicrobial activity of the new substance remained approximately at the same level.
format Article
id doaj-art-f8e027d1c0eb45bda3590dbd60cfdfea
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issn 0235-2990
language Russian
publishDate 2020-05-01
publisher LLC "Publishing House OKI"
record_format Article
series Антибиотики и Химиотерапия
spelling doaj-art-f8e027d1c0eb45bda3590dbd60cfdfea2025-08-20T02:49:36ZrusLLC "Publishing House OKI"Антибиотики и Химиотерапия0235-29902020-05-01637-841088Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and TriindolylmethanesS. N. Lavrenov0A. Yu. Simonov1A. A. Panov2S. A. Lakatosh3E. B. Isakova4E. A. Tsvigun5O. P. Bychkova6V. V. Tatarskiy7E. S. Ivanova8E. P. Mirchink9A. M. Korolev10A. S'. Trenin11Gause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsN. N. Blokhin National Medical Recearch Center of Oncology of the Ministry of Health of the Russian FederationN. N. Blokhin National Medical Recearch Center of Oncology of the Ministry of Health of the Russian FederationGause Institute of New AntibioticsGause Institute of New AntibioticsGause Institute of New AntibioticsMethods for the synthesis of hybrid molecules that combine the structure of a highly active antimicrobial compounds - tris(1-alkylindol-3-yl)methylium as well as 3-(indol-1-yl)maleimides that previously showed activity against some protein kinases have been developed. The main purpose of this study was to investigate the influence of substituents on the activity of compounds against different test microorganisms, as well as their toxicity on human cells. For example, with the introduction of a fragment of maleimide, it was possible to reduce cytotoxicity by almost 40 times compared to the original prototype in some cases. At the same time, antimicrobial activity of the new substance remained approximately at the same level.https://www.antibiotics-chemotherapy.ru/jour/article/view/89hybrid antibioticstriindolylmethane derivativesmaleimideschemical synthesisantibacterial and antifungal activity in vitrorelations between structure and biological activity
spellingShingle S. N. Lavrenov
A. Yu. Simonov
A. A. Panov
S. A. Lakatosh
E. B. Isakova
E. A. Tsvigun
O. P. Bychkova
V. V. Tatarskiy
E. S. Ivanova
E. P. Mirchink
A. M. Korolev
A. S'. Trenin
Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
Антибиотики и Химиотерапия
hybrid antibiotics
triindolylmethane derivatives
maleimides
chemical synthesis
antibacterial and antifungal activity in vitro
relations between structure and biological activity
title Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
title_full Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
title_fullStr Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
title_full_unstemmed Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
title_short Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes
title_sort synthesis and biological activity of new antimicrobial agents hybrid derivatives of maleimides and triindolylmethanes
topic hybrid antibiotics
triindolylmethane derivatives
maleimides
chemical synthesis
antibacterial and antifungal activity in vitro
relations between structure and biological activity
url https://www.antibiotics-chemotherapy.ru/jour/article/view/89
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