4-cyanopirazoles derivatives as a new class of compounds with potent antifungal activity

Risultato della ricerca: Conference article

Abstract

IntroductionWe have reported that some 4-nitrosopyrazoles derivatives displayed invitro and in vivo potent antifungal activity at no cytotoxic concentrationand some of these compounds were 4 times more potent thanAmphotericine B and Fluconazole respectively against CryptococcusNeoformans and C. Krusei.We reported also that the absence of NO group or its replacement withNO2 or NH2 groups gave compounds devoid of antimycotical activity.Aim of the workTo better understand the mechanism of action and with the aim ofidentifying the chemical features responsible for the action, wesynthesized and tested a new class of compounds in which the 4-NO groupwas replaced with 4-CN group having, these last, similar steric andelectronic features, but different routes by which may be metabolized invivo.ResultThe title compounds tested in vitro for antifungal activity against C.Neoformans and C. Krusei, displayed an interesting antifungal activity,increased compared to the analogous 4-NO-pyrazoles
Lingua originaleEnglish
Numero di pagine1
RivistaJOURNAL OF BIOLOGICAL RESEARCH
Stato di pubblicazionePublished - 2015

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Pyrazoles
Fluconazole
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@article{f7eb7dcfb8a44e0d9bbd10a667382e8c,
title = "4-cyanopirazoles derivatives as a new class of compounds with potent antifungal activity",
abstract = "IntroductionWe have reported that some 4-nitrosopyrazoles derivatives displayed invitro and in vivo potent antifungal activity at no cytotoxic concentrationand some of these compounds were 4 times more potent thanAmphotericine B and Fluconazole respectively against CryptococcusNeoformans and C. Krusei.We reported also that the absence of NO group or its replacement withNO2 or NH2 groups gave compounds devoid of antimycotical activity.Aim of the workTo better understand the mechanism of action and with the aim ofidentifying the chemical features responsible for the action, wesynthesized and tested a new class of compounds in which the 4-NO groupwas replaced with 4-CN group having, these last, similar steric andelectronic features, but different routes by which may be metabolized invivo.ResultThe title compounds tested in vitro for antifungal activity against C.Neoformans and C. Krusei, displayed an interesting antifungal activity,increased compared to the analogous 4-NO-pyrazoles",
author = "Fabio Venturella and Stefania Aiello",
year = "2015",
language = "English",
journal = "JOURNAL OF BIOLOGICAL RESEARCH",
issn = "2284-0230",

}

TY - JOUR

T1 - 4-cyanopirazoles derivatives as a new class of compounds with potent antifungal activity

AU - Venturella, Fabio

AU - Aiello, Stefania

PY - 2015

Y1 - 2015

N2 - IntroductionWe have reported that some 4-nitrosopyrazoles derivatives displayed invitro and in vivo potent antifungal activity at no cytotoxic concentrationand some of these compounds were 4 times more potent thanAmphotericine B and Fluconazole respectively against CryptococcusNeoformans and C. Krusei.We reported also that the absence of NO group or its replacement withNO2 or NH2 groups gave compounds devoid of antimycotical activity.Aim of the workTo better understand the mechanism of action and with the aim ofidentifying the chemical features responsible for the action, wesynthesized and tested a new class of compounds in which the 4-NO groupwas replaced with 4-CN group having, these last, similar steric andelectronic features, but different routes by which may be metabolized invivo.ResultThe title compounds tested in vitro for antifungal activity against C.Neoformans and C. Krusei, displayed an interesting antifungal activity,increased compared to the analogous 4-NO-pyrazoles

AB - IntroductionWe have reported that some 4-nitrosopyrazoles derivatives displayed invitro and in vivo potent antifungal activity at no cytotoxic concentrationand some of these compounds were 4 times more potent thanAmphotericine B and Fluconazole respectively against CryptococcusNeoformans and C. Krusei.We reported also that the absence of NO group or its replacement withNO2 or NH2 groups gave compounds devoid of antimycotical activity.Aim of the workTo better understand the mechanism of action and with the aim ofidentifying the chemical features responsible for the action, wesynthesized and tested a new class of compounds in which the 4-NO groupwas replaced with 4-CN group having, these last, similar steric andelectronic features, but different routes by which may be metabolized invivo.ResultThe title compounds tested in vitro for antifungal activity against C.Neoformans and C. Krusei, displayed an interesting antifungal activity,increased compared to the analogous 4-NO-pyrazoles

UR - http://hdl.handle.net/10447/158999

M3 - Conference article

JO - JOURNAL OF BIOLOGICAL RESEARCH

JF - JOURNAL OF BIOLOGICAL RESEARCH

SN - 2284-0230

ER -