Literature DB >> 29203486

In Vitro, In Silico, and In Vivo Analyses of Novel Aromatic Amidines against Trypanosoma cruzi.

Camila C Santos1, Jéssica R Lionel1, Raiza B Peres1, Marcos M Batista1, Patrícia B da Silva1, Gabriel M de Oliveira1, Cristiane F da Silva1, Denise G J Batista1, Sandra Maria O Souza2, Carolina H Andrade3, Bruno J Neves3, Rodolpho C Braga3, Donald A Patrick4, Svetlana M Bakunova4, Richard R Tidwell4, Maria de Nazaré C Soeiro5.   

Abstract

Five bis-arylimidamides were assayed as anti-Trypanosoma cruzi agents by in vitro, in silico, and in vivo approaches. None were considered to be pan-assay interference compounds. They had a favorable pharmacokinetic landscape and were active against trypomastigotes and intracellular forms, and in combination with benznidazole, they gave no interaction. The most selective agent (28SMB032) tested in vivo led to a 40% reduction in parasitemia (0.1 mg/kg of body weight/5 days intraperitoneally) but without mortality protection. In silico target fishing suggested DNA as the main target, but ultrastructural data did not match.
Copyright © 2018 American Society for Microbiology.

Entities:  

Keywords:  Chagas disease; arylimidamides; experimental chemotherapy; in vivo

Mesh：

Substances：

Year:  2018        PMID： 29203486      PMCID： PMC5786784          DOI： 10.1128/AAC.02205-17

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  29 in total

1.  Arylimidamide DB766, a potential chemotherapeutic candidate for Chagas' disease treatment.

Authors:  Denise da Gama Jaén Batista; Marcos Meuser Batista; Gabriel Melo de Oliveira; Patrícia Borges do Amaral; Joseli Lannes-Vieira; Constança Carvalho Britto; Angela Junqueira; Marli Maria Lima; Alvaro José Romanha; Policarpo Ademar Sales Junior; Chad E Stephens; David W Boykin; Maria de Nazaré Correia Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2010-05-10       Impact factor: 5.191

2.  Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.

Authors:  C E Stephens; F Tanious; S Kim; W D Wilson; W A Schell; J R Perfect; S G Franzblau; D W Boykin
Journal:  J Med Chem       Date:  2001-05-24       Impact factor: 7.446

3.  Modified fixed-ratio isobologram method for studying in vitro interactions between atovaquone and proguanil or dihydroartemisinin against drug-resistant strains of Plasmodium falciparum.

Authors:  Quinton L Fivelman; Ipemida S Adagu; David C Warhurst
Journal:  Antimicrob Agents Chemother       Date:  2004-11       Impact factor: 5.191

4.  [Various pyrazole and isoxazole derivatives with tuberculostatic action].

Authors:  C MUSANTE
Journal:  Farmaco Sci Tec       Date:  1951 Jan-Feb

5.  Benchmark data set for in silico prediction of Ames mutagenicity.

Authors:  Katja Hansen; Sebastian Mika; Timon Schroeter; Andreas Sutter; Antonius ter Laak; Thomas Steger-Hartmann; Nikolaus Heinrich; Klaus-Robert Müller
Journal:  J Chem Inf Model       Date:  2009-09       Impact factor: 4.956

6.  New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays.

Authors:  Jonathan B Baell; Georgina A Holloway
Journal:  J Med Chem       Date:  2010-04-08       Impact factor: 7.446

7.  In vitro and in vivo experimental models for drug screening and development for Chagas disease.

Authors:  Alvaro José Romanha; Solange Lisboa de Castro; Maria de Nazaré Correia Soeiro; Joseli Lannes-Vieira; Isabela Ribeiro; André Talvani; Bernadette Bourdin; Bethania Blum; Bianca Olivieri; Carlos Zani; Carmenza Spadafora; Egler Chiari; Eric Chatelain; Gabriela Chaves; José Eduardo Calzada; Juan Manuel Bustamante; Lucio H Freitas-Junior; Luz I Romero; Maria Terezinha Bahia; Michel Lotrowska; Milena Soares; Sonia Gumes Andrade; Tanya Armstrong; Wim Degrave; Zilton de Araújo Andrade
Journal:  Mem Inst Oswaldo Cruz       Date:  2010-03       Impact factor: 2.743

8.  A mechanism for cross-resistance to nifurtimox and benznidazole in trypanosomes.

Authors:  Shane R Wilkinson; Martin C Taylor; David Horn; John M Kelly; Ian Cheeseman
Journal:  Proc Natl Acad Sci U S A       Date:  2008-03-26       Impact factor: 11.205

9.  Molecular probes for imaging myelinated white matter in CNS.

Authors:  Chunying Wu; Jinjun Wei; Donghua Tian; Yue Feng; Robert H Miller; Yanming Wang
Journal:  J Med Chem       Date:  2008-10-10       Impact factor: 7.446

10.  Mucin-like molecules form a negatively charged coat that protects Trypanosoma cruzi trypomastigotes from killing by human anti-alpha-galactosyl antibodies.

Authors:  V L Pereira-Chioccola; A Acosta-Serrano; I Correia de Almeida; M A Ferguson; T Souto-Padron; M M Rodrigues; L R Travassos; S Schenkman
Journal:  J Cell Sci       Date:  2000-04       Impact factor: 5.285
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  4 in total

1.  Imidazole Derivatives as Promising Agents for the Treatment of Chagas Disease.

Authors:  Julianna Siciliano de Araújo; Alfonso García-Rubia; Victor Sebastián-Pérez; Titilola D Kalejaiye; Patrícia Bernardino da Silva; Cristina Rosa Fonseca-Berzal; Louis Maes; Harry P De Koning; Maria de Nazaré Correia Soeiro; Carmen Gil
Journal:  Antimicrob Agents Chemother       Date:  2019-03-27       Impact factor: 5.191

2.  In Vitro and In Vivo Evaluation of an Adamantyl-Based Phenyl Sulfonyl Acetamide against Cutaneous Leishmaniasis Models of Leishmania amazonensis.

Authors:  Camila C Santos; Huaisheng Zhang; Marcos M Batista; Gabriel M de Oliveira; Kelly C Demarque; Natália L da Silva-Gomes; Otacílio C Moreira; Ifedayo Victor Ogungbe; Maria de Nazaré C Soeiro
Journal:  Antimicrob Agents Chemother       Date:  2020-11-17       Impact factor: 5.191

3.  Differentiating Trypanosoma cruzi in a Host Mammalian Cell Imaged in Aqueous Liquid by Atmospheric Scanning Electron Microscopy.

Authors:  Yuko Takagi; Mari Sato; Masami Naya; Chikara Sato
Journal:  Microbiol Spectr       Date:  2022-01-05

4.  7-Aryl-7-deazapurine 3'-deoxyribonucleoside derivative as a novel lead for Chagas' disease therapy: in vitro and in vivo pharmacology.

Authors:  Camila Cardoso-Santos; Ludmila Ferreira de Almeida Fiuza; Cristiane França da Silva; Ana Lia Mazzeti; Roberson Donola Girão; Gabriel Melo de Oliveira; Denise da Gama Jaen Batista; Otacilio Cruz Moreira; Natália Lins da Silva Gomes; Louis Maes; Guy Caljon; Fabian Hulpia; Serge V Calenbergh; Maria de Nazaré Correia Soeiro
Journal:  JAC Antimicrob Resist       Date:  2021-11-17
  4 in total

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