Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action

Béla Kocsis; Ildikó Kustos; Ferenc Kilár; Adrien Nyul; Péter B. Jakus; Szilárd Kerekes; Victor Villarreal; László Prókai; Tamás Lóránd

doi:10.1016/j.ejmech.2008.10.038

Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action

Béla Kocsis, Ildikó Kustos, Ferenc Kilár, Adrien Nyul, Péter B. Jakus, Szilárd Kerekes, Victor Villarreal, László Prókai, Tamás Lóránd

Research output: Contribution to journal › Article › peer-review

16 Scopus citations

Abstract

The antifungal activity of some known unsaturated Mannich ketones and their amino alcohols has been reported and the mechanism of antifungal action has been studied. The inhibition of the fungal ergosterol, chitin, protein synthesis and pseudohypha formation was investigated. According to our results, Mannich ketones can influence the development of pseudohyphae of Candida albicans strains. In addition, they are able to induce significant changes in the protein composition of this fungal strain. Some of our Mannich ketones have shown inhibitory effect on the fungal chitin synthase enzyme. QSAR studies were also carried out.

Original language	English
Pages (from-to)	1823-1829
Number of pages	7
Journal	European Journal of Medicinal Chemistry
Volume	44
Issue number	5
DOIs	https://doi.org/10.1016/j.ejmech.2008.10.038
State	Published - May 2009

Keywords

Antifungal activity
Chitin synthase
Mannich ketone
Protein synthesis
Pseudohypha
QSAR

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10.1016/j.ejmech.2008.10.038

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@article{09a1e177dabe4239bee676620309ca17,

title = "Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action",

abstract = "The antifungal activity of some known unsaturated Mannich ketones and their amino alcohols has been reported and the mechanism of antifungal action has been studied. The inhibition of the fungal ergosterol, chitin, protein synthesis and pseudohypha formation was investigated. According to our results, Mannich ketones can influence the development of pseudohyphae of Candida albicans strains. In addition, they are able to induce significant changes in the protein composition of this fungal strain. Some of our Mannich ketones have shown inhibitory effect on the fungal chitin synthase enzyme. QSAR studies were also carried out.",

keywords = "Antifungal activity, Chitin synthase, Mannich ketone, Protein synthesis, Pseudohypha, QSAR",

author = "B{\'e}la Kocsis and Ildik{\'o} Kustos and Ferenc Kil{\'a}r and Adrien Nyul and Jakus, {P{\'e}ter B.} and Szil{\'a}rd Kerekes and Victor Villarreal and L{\'a}szl{\'o} Pr{\'o}kai and Tam{\'a}s L{\'o}r{\'a}nd",

note = "Funding Information: The work was supported by the grants GVOP-3.2.1-0168 and RET 008-2005. L{\'a}szl{\'o} Pr{\'o}kai is the Robert A. Welch Professor of the University of North Texas Health Science Center (grant number BK-0031). The authors thank Mrs. Erika Kocsis and Mrs. Krisztina Sajti for their technical assistance.",

year = "2009",

month = may,

doi = "10.1016/j.ejmech.2008.10.038",

language = "English",

volume = "44",

pages = "1823--1829",

journal = "European Journal of Medicinal Chemistry",

issn = "0223-5234",

publisher = "Elsevier Masson SAS",

number = "5",

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TY - JOUR

T1 - Antifungal unsaturated cyclic Mannich ketones and amino alcohols

T2 - Study of mechanism of action

AU - Kocsis, Béla

AU - Kustos, Ildikó

AU - Kilár, Ferenc

AU - Nyul, Adrien

AU - Jakus, Péter B.

AU - Kerekes, Szilárd

AU - Villarreal, Victor

AU - Prókai, László

AU - Lóránd, Tamás

N1 - Funding Information: The work was supported by the grants GVOP-3.2.1-0168 and RET 008-2005. László Prókai is the Robert A. Welch Professor of the University of North Texas Health Science Center (grant number BK-0031). The authors thank Mrs. Erika Kocsis and Mrs. Krisztina Sajti for their technical assistance.

PY - 2009/5

Y1 - 2009/5

N2 - The antifungal activity of some known unsaturated Mannich ketones and their amino alcohols has been reported and the mechanism of antifungal action has been studied. The inhibition of the fungal ergosterol, chitin, protein synthesis and pseudohypha formation was investigated. According to our results, Mannich ketones can influence the development of pseudohyphae of Candida albicans strains. In addition, they are able to induce significant changes in the protein composition of this fungal strain. Some of our Mannich ketones have shown inhibitory effect on the fungal chitin synthase enzyme. QSAR studies were also carried out.

AB - The antifungal activity of some known unsaturated Mannich ketones and their amino alcohols has been reported and the mechanism of antifungal action has been studied. The inhibition of the fungal ergosterol, chitin, protein synthesis and pseudohypha formation was investigated. According to our results, Mannich ketones can influence the development of pseudohyphae of Candida albicans strains. In addition, they are able to induce significant changes in the protein composition of this fungal strain. Some of our Mannich ketones have shown inhibitory effect on the fungal chitin synthase enzyme. QSAR studies were also carried out.

KW - Antifungal activity

KW - Chitin synthase

KW - Mannich ketone

KW - Protein synthesis

KW - Pseudohypha

KW - QSAR

UR - http://www.scopus.com/inward/record.url?scp=62749100520&partnerID=8YFLogxK

U2 - 10.1016/j.ejmech.2008.10.038

DO - 10.1016/j.ejmech.2008.10.038

M3 - Article

C2 - 19084292

AN - SCOPUS:62749100520

SN - 0223-5234

VL - 44

SP - 1823

EP - 1829

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

IS - 5

ER -

Antifungal unsaturated cyclic Mannich ketones and amino alcohols: Study of mechanism of action

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Keywords

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