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Journal of Enzyme Inhibition and Medicinal Chemistry Volume 25, 2010 - Issue 1
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Research Article

Cruzain inhibition by hydroxymethylnitrofurazone and nitrofurazone: investigation of a new target in Trypanosoma cruzi

Gustavo H. G. TrossiniDepartamento de Farmácia, Faculdade de Ciências Farmacêuticas, USP, São Paulo, BrazilCorrespondence[email protected]
,
Alberto MalvezziDepartamento de Química Fundamental, Instituto de Química, USP, São Paulo, Brazil
,
Antonia T.-do AmaralDepartamento de Química Fundamental, Instituto de Química, USP, São Paulo, Brazil
,
Carlota Oliveira Rangel-YaguiDepartamento de Farmácia, Faculdade de Ciências Farmacêuticas, USP, São Paulo, Brazil
,
Mario A. IzidoroDepartamento de Biofísica, INFAR, Escola Paulista de Medicina, UNIFESP, São Paulo, Brazil
,
Maria Helena S. CezariDepartamento de Biofísica, INFAR, Escola Paulista de Medicina, UNIFESP, São Paulo, Brazil
,
Luiz JulianoDepartamento de Biofísica, INFAR, Escola Paulista de Medicina, UNIFESP, São Paulo, Brazil
,
Chung Man ChinFaculdade de Ciências Farmacêutica, UNESP, São Paulo, Brazil
,
Carla M. S. MenezesDepartamento de Farmácia, Faculdade de Ciências Farmacêuticas, USP, São Paulo, Brazil
&
Elizabeth Igne FerreiraDepartamento de Farmácia, Faculdade de Ciências Farmacêuticas, USP, São Paulo, Brazil
 show all
Pages 62-67 | Received 09 Dec 2008, Accepted 26 Mar 2009, Published online: 23 Dec 2009

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Daniel Gedder Silva, Josmar Rodrigues Rocha, Geraldo Rodrigues Sartori & Carlos Alberto Montanari. (2017) Highly predictive hologram QSAR models of nitrile-containing cruzain inhibitors. Journal of Biomolecular Structure and Dynamics 35:15, pages 3232-3249.
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Drielli G. Vital, Flávia S. Damasceno, Ludmila N. Rapado, Ariel M. Silber, Filipe S. Vilella, Rafaela S. Ferreira, Vinícius G. Maltarollo & Gustavo H. G. Trossini. (2017) Application of bioisosterism in design of the semicarbazone derivatives as cruzain inhibitors: a theoretical and experimental study. Journal of Biomolecular Structure and Dynamics 35:6, pages 1244-1259.
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Articles from other publishers (20)

Diego B. Carvalho, Amarith R. das Neves, Gisele B. Portapilla, Ozildeia Soares, Larissa B. B. Santos, Jefferson R. S. Oliveira, Luan S. Vianna, Wagner A. S. Judice, Iara A. Cardoso, Pedro H. Luccas, M. Cristina Nonato, Norberto P. Lopes, Sergio de Albuquerque & Adriano C. M. Baroni. (2022) Repurposing of 5‐nitrofuran‐3,5‐disubstituted isoxazoles: A thriving scaffold to antitrypanosomal agents. Archiv der Pharmazie.
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Soraya S. Santos, Rodrigo V. Gonzaga, Cauê B. Scarim, Jeanine Giarolla, Marina C. Primi, Chung M. Chin & Elizabeth I. Ferreira. (2022) Drug/Lead Compound Hydroxymethylation as a Simple Approach to Enhance Pharmacodynamic and Pharmacokinetic Properties. Frontiers in Chemistry 9.
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Marwa H. El-Wakil, Marwa Ahmed Meheissen & Marwa M. Abu-Serie. (2021) Nitrofurazone repurposing towards design and synthesis of novel apoptotic-dependent anticancer and antimicrobial agents: Biological evaluation, kinetic studies and molecular modeling. Bioorganic Chemistry 113, pages 104971.
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Natália N. Santiago, Giulianna P. de Alcântara, Juliana S. da Costa, Samir A. Carvalho, Juliana M.C. Barbosa, Kelly Salomão, Solange L. de Castro, Henrique M.G. Pereira & Edson F. da Silva. (2020) Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives. Medicinal Chemistry 16:4, pages 487-494.
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Nonkululeko H. Zuma, Janine Aucamp & David D. N'Da. (2019) An update on derivatisation and repurposing of clinical nitrofuran drugs. European Journal of Pharmaceutical Sciences 140, pages 105092.
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Cauê Benito Scarim & Chung Man Chin. (2019) Nitroheterocyclic derivatives: privileged scaffold for drug development against Chagas disease. Medicinal Chemistry Research 28:12, pages 2099-2108.
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Cauê B. Scarim, Cleverton R. de Andrade, João A. da Rosa, Jean L. dos Santos & Chung M. Chin. (2018) Hydroxymethylnitrofurazone treatment in indeterminate form of chronic Chagas disease: Reduced intensity of tissue parasitism and inflammation-A histopathological study. International Journal of Experimental Pathology 99:5, pages 236-248.
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Cauê Benito Scarim, Daniela Hartmann Jornada, Rafael Consolin Chelucci, Leticia de Almeida, Jean Leandro dos Santos & Man Chin Chung. (2018) Current advances in drug discovery for Chagas disease. European Journal of Medicinal Chemistry 155, pages 824-838.
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Luisa Donatto Chiavassa & Mauro Aquiles La-Scalea. (2017) Square wave voltammetry of nitrofurans in aqueous media using a carbon fiber microelectrode. Journal of Solid State Electrochemistry 22:5, pages 1395-1402.
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Anacleto S. de Souza, Marcelo T. de Oliveira & Adriano D. Andricopulo. (2017) Development of a pharmacophore for cruzain using oxadiazoles as virtual molecular probes: quantitative structure–activity relationship studies. Journal of Computer-Aided Molecular Design 31:9, pages 801-816.
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Fredson T. Silva, Caio H. Franco, Denize C. Favaro, Lucio H. Freitas-Junior, Carolina B. Moraes & Elizabeth I. Ferreira. (2016) Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues. European Journal of Medicinal Chemistry 121, pages 553-560.
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José Bermudez, Carolina Davies, Analía Simonazzi, Juan Pablo Real & Santiago Palma. (2016) Current drug therapy and pharmaceutical challenges for Chagas disease. Acta Tropica 156, pages 1-16.
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José Wanderlan Pontes Espíndola, Marcos Veríssimo de Oliveira Cardoso, Gevanio Bezerra de Oliveira Filho, Dayane Albuquerque Oliveira e Silva, Diogo Rodrigo Magalhaes Moreira, Tanira Matutino Bastos, Carlos Alberto de Simone, Milena Botelho Pereira Soares, Filipe Silva Villela, Rafaela Salgado Ferreira, Maria Carolina Accioly Brelaz de Castro, Valéria Rego Alves Pereira, Silvane Maria Fonseca Murta, Policarpo Ademar Sales Junior, Alvaro José Romanha & Ana Cristina Lima Leite. (2015) Synthesis and structure–activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain. European Journal of Medicinal Chemistry 101, pages 818-835.
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Carolina Davies, Nilay Dey, Olga Sanchez Negrette, Luis Antonio Parada, Miguel A. Basombrio & Nisha Jain Garg. (2014) Hepatotoxicity in Mice of a Novel Anti-parasite Drug Candidate Hydroxymethylnitrofurazone: A Comparison with Benznidazole. PLoS Neglected Tropical Diseases 8:10, pages e3231.
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Diogo Rodrigo Magalhaes Moreira, Ana Daura Travassos de Oliveira, Paulo André Teixeira de Moraes Gomes, Carlos Alberto de Simone, Filipe Silva Villela, Rafaela Salgado Ferreira, Aline Caroline da Silva, Thiago André Ramos dos Santos, Maria Carolina Accioly Brelaz de Castro, Valéria Rego Alves Pereira & Ana Cristina Lima Leite. (2014) Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death. European Journal of Medicinal Chemistry 75, pages 467-478.
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Lorena Blau, Renato Farina Menegon, Gustavo H.G. Trossini, João Vitor Dutra Molino, Drielli Gomes Vital, Regina Maria Barretto Cicarelli, Gabriela Duó Passerini, Priscila Longhin Bosquesi & Chung Man Chin. (2013) Design, synthesis and biological evaluation of new aryl thiosemicarbazone as antichagasic candidates. European Journal of Medicinal Chemistry 67, pages 142-151.
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Yongnian Ni, Pingping Wang & Serge Kokot. (2012) Voltammetric investigation of DNA damage induced by nitrofurazone and short-lived nitro-radicals with the use of an electrochemical DNA biosensor. Biosensors and Bioelectronics 38:1, pages 245-251.
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Carla M. S. Menezes, Gildardo Rivera, Marina A. Alves, Daniel N. do Amaral, Jean Pierre B. Thibaut, François Noël, Eliezer J. Barreiro & Lídia M. Lima. (2012) Synthesis, Biological Evaluation, and Structure-activity Relationship of Clonazepam, Meclonazepam, and 1,4-Benzodiazepine Compounds with Schistosomicidal Activity. Chemical Biology & Drug Design 79:6, pages 943-949.
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Marcelo Zaldini Hernandes, Marcelo Montenegro Rabello, Ana Cristina Lima Leite, Marcos Veríssimo Oliveira Cardoso, Diogo Rodrigo Magalhaes Moreira, Dalci José Brondani, Carlos Alberto Simone, Luiza Campos Reis, Marina Assis Souza, Valéria Rego Alves Pereira, Rafaela Salgado Ferreira & James Hobson McKerrow. (2010) Studies toward the structural optimization of novel thiazolylhydrazone-based potent antitrypanosomal agents. Bioorganic & Medicinal Chemistry 18:22, pages 7826-7835.
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Hugo Cerecetto & Mercedes González. (2010) Synthetic Medicinal Chemistry in Chagas’ Disease: Compounds at The Final Stage of “Hit-To-Lead” Phase. Pharmaceuticals 3:4, pages 810-838.
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