KFU. Card publication. Elucidation of the Mode of Action of New Antibacterial Bis-Phosphonium Salts of Pyridine Derivatives Active Against Staphylococcus aureus

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ELUCIDATION OF THE MODE OF ACTION OF NEW ANTIBACTERIAL BIS-PHOSPHONIUM SALTS OF PYRIDINE DERIVATIVES ACTIVE AGAINST STAPHYLOCOCCUS AUREUS

Form of presentation

Articles in international journals and collections

Year of publication

2017

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Authors, employees of KFU

Vafina Ruzaliya Maskhutovna, author

Evtyugin Vladimir Gennadevich, author

Zeldi Marina Ivanovna, author

Kayumov Ayrat Rashitovich, author

Nikitina Elena Vladimirovna, author

Pugachev Mikhail Vladimirovich, author

Fedosimova Svetlana Vladimirovna, author

Shtyrlin Nikita Valerevich, author

Shtyrlin Yuriy Grigorevich, author

Bibliographic description in the original language

Nikitina E.V. Elucidation of the Mode of Action of New Antibacterial Bis-Phosphonium Salts of Pyridine Derivatives Active Against Staphylococcus aureus / E.V. Nikitina, M.I. Zeldi, R.M. Vafina, M.V. Pugachev, N.V. Shtyrlin, S.V. Kuznetsova, V.G. Evtugyn, A.R. Kayumov, Y.G. Shtyrlin // RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES. - 2017. - V.8, Is.3. - P.1906-1915.

Annotation

In this study, we show the antibacterial activity of a new group of antimicrobial compounds, quaternary bis-phosphonium salts of pyridine derivatives synthesized previously in our group. These compounds exhibit broad-spectrum of antibacterial activity against gram-positive bacteria including methicillin-resistant strains of Staphylococcus aureus. By using both scanning and transmission electron microscopy we found that the lead compound 6-Bis[(tri-p-tolylphosphonio)methyl]-3-hydroxypyridin-1-ium trichloride (2a) bearing two p-tolyl substituents at the phosphorus atoms exhibits a highest antibacterial activity and affects the cell wall of S. aureus, which results in filamentous growth, roughened surface of cells with excrescences and unusual protrusions. While the confocal scanning microscopy showed only partial loss of membrane integrity at 1×MIC of 2a, TEM studies revealed that 2a exerts cell wall damage resulting in breaks and diffuse structure of peptidoglycan layer, which is likely

Keywords

quaternary phosphonium salts, pyridine, antibacterial activity, microscopy

The name of the journal

RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES

URL

https://www.rjpbcs.com/pdf/2017_8(3)/[223].pdf

Please use this ID to quote from or refer to the card

https://repository.kpfu.ru/eng/?p_id=168670&p_lang=2

Full metadata record

Field DC	Value	Language
dc.contributor.author	Vafina Ruzaliya Maskhutovna	ru_RU
dc.contributor.author	Evtyugin Vladimir Gennadevich	ru_RU
dc.contributor.author	Zeldi Marina Ivanovna	ru_RU
dc.contributor.author	Kayumov Ayrat Rashitovich	ru_RU
dc.contributor.author	Nikitina Elena Vladimirovna	ru_RU
dc.contributor.author	Pugachev Mikhail Vladimirovich	ru_RU
dc.contributor.author	Fedosimova Svetlana Vladimirovna	ru_RU
dc.contributor.author	Shtyrlin Nikita Valerevich	ru_RU
dc.contributor.author	Shtyrlin Yuriy Grigorevich	ru_RU
dc.date.accessioned	2017-01-01T00:00:00Z	ru_RU
dc.date.available	2017-01-01T00:00:00Z	ru_RU
dc.date.issued	2017	ru_RU
dc.identifier.citation	Nikitina E.V. Elucidation of the Mode of Action of New Antibacterial Bis-Phosphonium Salts of Pyridine Derivatives Active Against Staphylococcus aureus / E.V. Nikitina, M.I. Zeldi, R.M. Vafina, M.V. Pugachev, N.V. Shtyrlin, S.V. Kuznetsova, V.G. Evtugyn, A.R. Kayumov, Y.G. Shtyrlin // RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES. - 2017. - V.8, Is.3. - P.1906-1915.	ru_RU
dc.identifier.uri	https://repository.kpfu.ru/eng/?p_id=168670&p_lang=2	ru_RU
dc.description.abstract	RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES	ru_RU
dc.description.abstract	In this study, we show the antibacterial activity of a new group of antimicrobial compounds, quaternary bis-phosphonium salts of pyridine derivatives synthesized previously in our group. These compounds exhibit broad-spectrum of antibacterial activity against gram-positive bacteria including methicillin-resistant strains of Staphylococcus aureus. By using both scanning and transmission electron microscopy we found that the lead compound 6-Bis[(tri-p-tolylphosphonio)methyl]-3-hydroxypyridin-1-ium trichloride (2a) bearing two p-tolyl substituents at the phosphorus atoms exhibits a highest antibacterial activity and affects the cell wall of S. aureus, which results in filamentous growth, roughened surface of cells with excrescences and unusual protrusions. While the confocal scanning microscopy showed only partial loss of membrane integrity at 1×MIC of 2a, TEM studies revealed that 2a exerts cell wall damage resulting in breaks and diffuse structure of peptidoglycan layer, which is likely	ru_RU
dc.language.iso	ru	ru_RU
dc.subject	quaternary phosphonium salts	ru_RU
dc.subject	pyridine	ru_RU
dc.subject	antibacterial activity	ru_RU
dc.subject	microscopy	ru_RU
dc.title	Elucidation of the Mode of Action of New Antibacterial Bis-Phosphonium Salts of Pyridine Derivatives Active Against Staphylococcus aureus	ru_RU
dc.type	Articles in international journals and collections	ru_RU