In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains

Charmina Aguirre-Alvarado; Fabiola Zaragoza-Martínez; Lorena Rodríguez-Páez; Benjamín Nogueda; Isabel Baeza; Carlos Wong

doi:10.1080/14756360601051233

In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains

Charmina Aguirre-Alvarado, Fabiola Zaragoza-Martínez, Lorena Rodríguez-Páez, Benjamín Nogueda, Isabel Baeza, Carlos Wong

Escuela Nacional de Ciencias Biológicas (ENCB)

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9 Scopus citations

Abstract

The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.

Original language	English
Pages (from-to)	227-233
Number of pages	7
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume	22
Issue number	2
DOIs	https://doi.org/10.1080/14756360601051233
State	Published - Apr 2007

Keywords

(α-hydroxyacid dehydrogenase (HADH)
(α-hydroxyacid dehydrogenase-isozyme II inhibition
Ethyl N-allyl oxamate
Ethyl N-propyl oxamate
Trypanosoma cruzi

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10.1080/14756360601051233

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@article{d789cd45ea4d475c85e1671228f9904f,

title = "In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains",

abstract = "The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.",

keywords = "(α-hydroxyacid dehydrogenase (HADH), (α-hydroxyacid dehydrogenase-isozyme II inhibition, Ethyl N-allyl oxamate, Ethyl N-propyl oxamate, Trypanosoma cruzi",

author = "Charmina Aguirre-Alvarado and Fabiola Zaragoza-Mart{\'i}nez and Lorena Rodr{\'i}guez-P{\'a}ez and Benjam{\'i}n Nogueda and Isabel Baeza and Carlos Wong",

note = "Funding Information: This work was partially supported by research grants from the Secretar{\'i}a de Investigaci{\'o}n y Posgrado del Instituto Polit{\'e}cnico Nacional (SIP-IPN), M{\'e}xico. C.W., L.R.P., B.N. and I.B. are fellows of the COFAA-IPN and of the SNI-CONACYT. Ch. A.A. and F.Z.M. are fellows of the CONACYT and PIFI-IPN.",

year = "2007",

month = apr,

doi = "10.1080/14756360601051233",

language = "Ingl{\'e}s",

volume = "22",

pages = "227--233",

journal = "Journal of Enzyme Inhibition and Medicinal Chemistry",

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In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains. / Aguirre-Alvarado, Charmina; Zaragoza-Martínez, Fabiola; Rodríguez-Páez, Lorena et al.
In: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 22, No. 2, 04.2007, p. 227-233.

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

TY - JOUR

T1 - In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains

AU - Aguirre-Alvarado, Charmina

AU - Zaragoza-Martínez, Fabiola

AU - Rodríguez-Páez, Lorena

AU - Nogueda, Benjamín

AU - Baeza, Isabel

AU - Wong, Carlos

N1 - Funding Information: This work was partially supported by research grants from the Secretaría de Investigación y Posgrado del Instituto Politécnico Nacional (SIP-IPN), México. C.W., L.R.P., B.N. and I.B. are fellows of the COFAA-IPN and of the SNI-CONACYT. Ch. A.A. and F.Z.M. are fellows of the CONACYT and PIFI-IPN.

PY - 2007/4

Y1 - 2007/4

N2 - The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.

AB - The trypanocidal activity of N-allyl (NAOx) and N-propyl (NPOx) oxamates and that of the ethyl esters of N-allyl (Et-NAOx) and N-propyl (Et-NPOx) oxamates were tested on cultured epimastigotes (in vitro) and murine trypanosomiasis (in vivo) using five different T. cruzi strains. NAOx and NPOx did not penetrate intact epimastigotes and therefore we were not able to detect any trypanocidal effect with these oxamates. Whereas the ethyl esters (Et-NAOx and Et-NPOx), acting as prodrugs, exhibited in vitro and in vivo trypanocidal activity on the five tested T. cruzi strains. On the contrary, when Nifurtimox and Benznidazole used as reference drugs were tested, we found that only three of the five tested T. cruzi strains were affected, whereas the other two strains, Miguz and Compostela, were resistant to the in vitro and in vivo trypanocidal activity of these compounds.

KW - (α-hydroxyacid dehydrogenase (HADH)

KW - (α-hydroxyacid dehydrogenase-isozyme II inhibition

KW - Ethyl N-allyl oxamate

KW - Ethyl N-propyl oxamate

KW - Trypanosoma cruzi

UR - http://www.scopus.com/inward/record.url?scp=34247131722&partnerID=8YFLogxK

U2 - 10.1080/14756360601051233

DO - 10.1080/14756360601051233

M3 - Artículo

SN - 1475-6366

VL - 22

SP - 227

EP - 233

JO - Journal of Enzyme Inhibition and Medicinal Chemistry

JF - Journal of Enzyme Inhibition and Medicinal Chemistry

IS - 2

ER -

In vitro and in vivo trypanocidal activity of the ethyl esters of N-allyl and N-propyl oxamates using different Trypanosoma cruzi strains

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Keywords

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