Literature DB >> 16483783

Indazole N-oxide derivatives as antiprotozoal agents: synthesis, biological evaluation and mechanism of action studies.

Alejandra Gerpe1, Gabriela Aguirre, Lucía Boiani, Hugo Cerecetto, Mercedes González, Claudio Olea-Azar, Carolina Rigol, Juan D Maya, Antonio Morello, Oscar E Piro, Vicente J Arán, Amaia Azqueta, Adela López de Ceráin, Antonio Monge, María Antonieta Rojas, Gloria Yaluff.   

Abstract

A series of indazole N-oxide derivatives have been synthesized and their antichagasic and leishmanocidal properties studied. 3-Cyano-2-(4-iodophenyl)-2H-indazole N1-oxide exhibited interesting antichagasic activity on the two parasitic strains and the two parasitic stages evaluated. Furthermore, besides its trypanocidal activity, 3-cyano-2-(4-nitrophenyl)-2H-indazole N1-oxide showed leishmanocidal activity in the three parasitic strains evaluated. To gain insight into the mechanism of action, electrochemical behaviour, ESR experiment, inhibition of parasitic respiration and QSAR were performed.

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Year:  2006        PMID： 16483783     DOI： 10.1016/j.bmc.2006.01.007

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

1.  Accessing Multiple Classes of 2 H-Indazoles: Mechanistic Implications for the Cadogan and Davis-Beirut Reactions.

Authors:  Jie S Zhu; Clarabella J Li; Ka Yi Tsui; Niklas Kraemer; Jung-Ho Son; Makhluf J Haddadin; Dean J Tantillo; Mark J Kurth
Journal:  J Am Chem Soc       Date:  2019-04-04       Impact factor: 15.419

2.  Remarkably efficient synthesis of 2H-indazole 1-oxides and 2H-indazoles via tandem carbon-carbon followed by nitrogen-nitrogen bond formation.

Authors:  Isabelle Bouillon; Jaroslav Zajícek; Nadĕzda Pudelová; Viktor Krchnák
Journal:  J Org Chem       Date:  2008-10-21       Impact factor: 4.354

Review 3.  1,4-naphthoquinones and other NADPH-dependent glutathione reductase-catalyzed redox cyclers as antimalarial agents.

Authors:  Didier Belorgey; Don Antoine Lanfranchi; Elisabeth Davioud-Charvet
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

4.  New hits as phase II enzymes inducers from a focused library with heteroatom-heteroatom and Michael-acceptor motives.

Authors:  Mauricio Cabrera; Stefani de Ovalle; Mariela Bollati-Fogolín; Fabiana Nascimento; Patrícia Corbelini; Fernanda Janarelli; Daniel Kawano; Vera Lucia Eifler-Lima; Mercedes González; Hugo Cerecetto
Journal:  Future Sci OA       Date:  2015-11-01

5.  Novel Azoles as Antiparasitic Remedies against Brain-Eating Amoebae.

Authors:  Ayaz Anwar; Mohammad Ridwane Mungroo; Simal Khan; Itrat Fatima; Rafaila Rafique; Khalid Mohammed Khan; Ruqaiyyah Siddiqui; Naveed Ahmed Khan
Journal:  Antibiotics (Basel)       Date:  2020-04-17

6.  Synthesis of N-phenyl- and N-thiazolyl-1H-indazoles by copper-catalyzed intramolecular N-arylation of ortho-chlorinated arylhydrazones.

Authors:  Yara Cristina Marchioro Barbosa; Guilherme Caneppele Paveglio; Claudio Martin Pereira de Pereira; Sidnei Moura; Cristiane Storck Schwalm; Gleison Antonio Casagrande; Lucas Pizzuti
Journal:  Beilstein J Org Chem       Date:  2022-08-23       Impact factor: 2.544

7.  Identification of potent chemotypes targeting Leishmania major using a high-throughput, low-stringency, computationally enhanced, small molecule screen.

Authors:  Elizabeth R Sharlow; David Close; Tongying Shun; Stephanie Leimgruber; Robyn Reed; Gabriela Mustata; Peter Wipf; Jacob Johnson; Michael O'Neil; Max Grögl; Alan J Magill; John S Lazo
Journal:  PLoS Negl Trop Dis       Date:  2009-11-03

Review 8.  Synthetic Medicinal Chemistry in Chagas' Disease: Compounds at The Final Stage of "Hit-To-Lead" Phase.

Authors:  Hugo Cerecetto; Mercedes González
Journal:  Pharmaceuticals (Basel)       Date:  2010-03-25
  8 in total

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