1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships
Hugo Cerecetto
1
,
Rossanna Di Maio
1
,
Mercedes Catalán González
1
,
Mariela Risso
1
,
PATRICIA SAENZ
1
,
Gustavo Seoane
1
,
Ana Denicola
1
,
Gonzalo Peluffo
1
,
Celia Quijano
1
,
Claudio Olea-Azar
1
Тип публикации: Journal Article
Дата публикации: 1999-05-06
scimago Q1
wos Q1
БС1
SJR: 1.801
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
10354402
Drug Discovery
Molecular Medicine
Краткое описание
The syntheses of a new series of derivatives of 1,2,5-oxadiazole N-oxide, benzo[1,2-c]1,2,5-oxadiazole N-oxide, and quinoxaline di-N-oxide are described. In vitro antitrypanosomal activity of these compounds was tested against epimastigote forms of Trypanosoma cruzi. For the most effective drugs, derivatives IIIe and IIIf, the 50% inhibitory dose (ID50) was determined as well as their cytotoxicity against mammalian fibroblasts. Electrochemical studies and ESR spectroscopy show that the highest activities observed are associated with the facile monoelectronation of the N-oxide moiety. Lipophilic-hydrophilic balance of the compounds could also play an important role in their effectiveness as antichagasic drugs.
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ГОСТ
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Cerecetto H. et al. 1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships // Journal of Medicinal Chemistry. 1999. Vol. 42. No. 11. pp. 1941-1950.
ГОСТ со всеми авторами (до 50)
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Cerecetto H., Di Maio R., González M. C., Risso M., SAENZ P., Seoane G., Denicola A., Peluffo G., Quijano C., Olea-Azar C. 1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships // Journal of Medicinal Chemistry. 1999. Vol. 42. No. 11. pp. 1941-1950.
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RIS
Скопировать
TY - JOUR
DO - 10.1021/jm9805790
UR - https://doi.org/10.1021/jm9805790
TI - 1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships
T2 - Journal of Medicinal Chemistry
AU - Cerecetto, Hugo
AU - Di Maio, Rossanna
AU - González, Mercedes Catalán
AU - Risso, Mariela
AU - SAENZ, PATRICIA
AU - Seoane, Gustavo
AU - Denicola, Ana
AU - Peluffo, Gonzalo
AU - Quijano, Celia
AU - Olea-Azar, Claudio
PY - 1999
DA - 1999/05/06
PB - American Chemical Society (ACS)
SP - 1941-1950
IS - 11
VL - 42
PMID - 10354402
SN - 0022-2623
SN - 1520-4804
ER -
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BibTex (до 50 авторов)
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@article{1999_Cerecetto,
author = {Hugo Cerecetto and Rossanna Di Maio and Mercedes Catalán González and Mariela Risso and PATRICIA SAENZ and Gustavo Seoane and Ana Denicola and Gonzalo Peluffo and Celia Quijano and Claudio Olea-Azar},
title = {1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships},
journal = {Journal of Medicinal Chemistry},
year = {1999},
volume = {42},
publisher = {American Chemical Society (ACS)},
month = {may},
url = {https://doi.org/10.1021/jm9805790},
number = {11},
pages = {1941--1950},
doi = {10.1021/jm9805790}
}
Цитировать
MLA
Скопировать
Cerecetto, Hugo, et al. “1,2,5-Oxadiazole N-Oxide Derivatives and Related Compounds as Potential Antitrypanosomal Drugs: Structure−Activity Relationships.” Journal of Medicinal Chemistry, vol. 42, no. 11, May. 1999, pp. 1941-1950. https://doi.org/10.1021/jm9805790.