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

Abstract

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.

About the Authors

S. N. Lavrenov
Gause Institute of New Antibiotics
Russian Federation


A. Yu. Simonov
Gause Institute of New Antibiotics
Russian Federation


A. A. Panov
Gause Institute of New Antibiotics
Russian Federation


S. A. Lakatosh
Gause Institute of New Antibiotics
Russian Federation


E. B. Isakova
Gause Institute of New Antibiotics
Russian Federation


E. A. Tsvigun
Gause Institute of New Antibiotics
Russian Federation


O. P. Bychkova
Gause Institute of New Antibiotics
Russian Federation


V. V. Tatarskiy
N. N. Blokhin National Medical Recearch Center of Oncology of the Ministry of Health of the Russian Federation
Russian Federation


E. S. Ivanova
N. N. Blokhin National Medical Recearch Center of Oncology of the Ministry of Health of the Russian Federation
Russian Federation


E. P. Mirchink
Gause Institute of New Antibiotics
Russian Federation


A. M. Korolev
Gause Institute of New Antibiotics
Russian Federation


A. S'. Trenin
Gause Institute of New Antibiotics
Russian Federation


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Review

For citations:


Lavrenov S.N., Simonov A.Yu., Panov A.A., Lakatosh S.A., Isakova E.B., Tsvigun E.A., Bychkova O.P., Tatarskiy V.V., Ivanova E.S., Mirchink E.P., Korolev A.M., Trenin A.S. Synthesis and Biological Activity of New Antimicrobial Agents - Hybrid Derivatives of Maleimides and Triindolylmethanes. Antibiot Khimioter = Antibiotics and Chemotherapy. 2018;63(7-8):4-10. (In Russ.)

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ISSN 0235-2990 (Print)