KFU. Card publication. New quaternary ammonium pyridoxine derivatives: synthesis and antibacterial activity

KAZAN
FEDERAL UNIVERSITY

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NEW QUATERNARY AMMONIUM PYRIDOXINE DERIVATIVES: SYNTHESIS AND ANTIBACTERIAL ACTIVITY

Form of presentation

Articles in international journals and collections

Year of publication

2017

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Authors, employees of KFU

Balakin Konstantin Valerevich, author

Bulatova Elena Sergeevna, author

Grishaev Denis Yurevich, author

Iksanova Alfiya Gabdulakhatovna, author

Kayumov Ayrat Rashitovich, author

Nikitina Elena Vladimirovna, author

Sapozhnikov Sergey Vitalevich, author

Shtyrlin Nikita Valerevich, author

Shtyrlin Yuriy Grigorevich, author

Authors, students KFU

Zamaldinova Alina Elbrusovna, author

Bibliographic description in the original language

Sapozhnikov S.V. New quaternary ammonium pyridoxine derivatives: synthesis and antibacterial activity / S.V. Sapozhnikov, N.V. Shtyrlin, A.R. Kayumov, A.E. Zamaldinova, A.G. Iksanova, E.V. Nikitina, E.S. Krylova, D.Yu. Grishaev, K.V. Balakin, Y.G. Shtyrlin // Medicinal Chemistry Research. - 2017. - V.26(12). - P. 3188-3202.

Annotation

A diverse library of 34 new quaternary mono-ammonium and bis-ammonium pyridoxine derivatives was synthesized, and their antibacterial activity against several clinically relevant bacterial strains was evaluated in vitro. Several mono-ammonium compounds demonstrated high antibacterial activity against methicillin-resistant Staphylococcus strains with minimum inhibitory concentrations in the range of 0.5–8 ?g/mL, which exceeded activity of miramistin and was comparable to that of benzalkonium chloride. SOS-chromotest in Salmonella typhimurium showed the lack of DNA-damage activity for all active compounds. A clear correlation has been observed between the lipophilicity of the obtained compounds and their activity against the studied Gram-positive bacterial strains. Cytotoxicity studies on HEK-293 cells demonstrated that some of the active compounds were less toxic than the reference drugs. Antibacterial activity studies in the presence of CaCl2 suggested that the cell wall damage associa

Keywords

Quaternary ammonium salts, Pyridoxine, Antibacterial activit,y Cytotoxicity, Genotoxicity, Cell wall damaging agents

The name of the journal

Medicinal Chemistry Research

URL

https://www.scopus.com/inward/record.uri?eid=2-s2.0-85028330282&doi=10.1007%2fs00044-017-2012-9&partnerID=40&md5=b0052601b01b79687ee14f788471aa44

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

https://repository.kpfu.ru/eng/?p_id=164444&p_lang=2

Full metadata record

Field DC	Value	Language
dc.contributor.author	Balakin Konstantin Valerevich	ru_RU
dc.contributor.author	Bulatova Elena Sergeevna	ru_RU
dc.contributor.author	Grishaev Denis Yurevich	ru_RU
dc.contributor.author	Iksanova Alfiya Gabdulakhatovna	ru_RU
dc.contributor.author	Kayumov Ayrat Rashitovich	ru_RU
dc.contributor.author	Nikitina Elena Vladimirovna	ru_RU
dc.contributor.author	Sapozhnikov Sergey Vitalevich	ru_RU
dc.contributor.author	Shtyrlin Nikita Valerevich	ru_RU
dc.contributor.author	Shtyrlin Yuriy Grigorevich	ru_RU
dc.contributor.author	Zamaldinova Alina Elbrusovna	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	Sapozhnikov S.V. New quaternary ammonium pyridoxine derivatives: synthesis and antibacterial activity / S.V. Sapozhnikov, N.V. Shtyrlin, A.R. Kayumov, A.E. Zamaldinova, A.G. Iksanova, �.V. Nikitina, �.S. Krylova, D.Yu. Grishaev, K.V. Balakin, Y.G. Shtyrlin // Medicinal Chemistry Research. - 2017. - V.26(12). - P. 3188-3202.	ru_RU
dc.identifier.uri	https://repository.kpfu.ru/eng/?p_id=164444&p_lang=2	ru_RU
dc.description.abstract	Medicinal Chemistry Research	ru_RU
dc.description.abstract	A diverse library of 34 new quaternary mono-ammonium and bis-ammonium pyridoxine derivatives was synthesized, and their antibacterial activity against several clinically relevant bacterial strains was evaluated in vitro. Several mono-ammonium compounds demonstrated high antibacterial activity against methicillin-resistant Staphylococcus strains with minimum inhibitory concentrations in the range of 0.5–8 ?g/mL, which exceeded activity of miramistin and was comparable to that of benzalkonium chloride. SOS-chromotest in Salmonella typhimurium showed the lack of DNA-damage activity for all active compounds. A clear correlation has been observed between the lipophilicity of the obtained compounds and their activity against the studied Gram-positive bacterial strains. Cytotoxicity studies on HEK-293 cells demonstrated that some of the active compounds were less toxic than the reference drugs. Antibacterial activity studies in the presence of CaCl2 suggested that the cell wall damage associa	ru_RU
dc.language.iso	ru	ru_RU
dc.subject	Quaternary ammonium salts	ru_RU
dc.subject	Pyridoxine	ru_RU
dc.subject	Antibacterial activit	ru_RU
dc.subject	y Cytotoxicity	ru_RU
dc.subject	Genotoxicity	ru_RU
dc.subject	Cell wall damaging agents	ru_RU
dc.title	New quaternary ammonium pyridoxine derivatives: synthesis and antibacterial activity	ru_RU
dc.type	Articles in international journals and collections	ru_RU