Abstract
Chagas disease (ChD), caused by Trypanosoma cruzi, remains a challenge for the medical and scientific fields due to the inefficiency of the therapeutic approaches available for its treatment. Thiosemicarbazones and hydrazones present a wide spectrum of bioactivities and are considered a platform for the design of new anti-T. cruzi drug candidates. Herein, the potential antichagasic activities of [(E)-2-(1-(4-chlorophenylthio)propan-2-ylidene)-hydrazinecarbothioamides] (C1, C3), [(E)-N'-(1-((4-chlorophenyl)thio)propan-2-ylidene)benzohydrazide] (C2), [(E)-2-(1-(4-, and [(E)-2-(1-((4-chlorophenyl)thio)propan-2-ylidene)hydrazinecarboxamide] (C4) were investigated. Macrophages (MOs) from C57BL/6 mice stimulated with C1 and C3, but not with C2 and C4, reduced amastigote replication and trypomastigote release, independent of nitric oxide (NO) and reactive oxygen species production and indoleamine 2,3-dioxygenase activity. C3, but not C1, reduced parasite uptake by MOs and potentiated TNF production. In cardiomyocytes, C3 reduced trypomastigote release independently of NO, TNF, and IL-6 production. C1 and C3 were non-toxic to the host cells. A reduction of parasite release was found during infection of MOs with trypomastigotes pre-incu...Continue Reading
References
Jan 1, 1978·Progress in Medicinal Chemistry·K C Agrawal, A C Sartorelli
Jan 1, 1992·Parasitology·B J Berger, A H Fairlamb
May 1, 1991·Infection and Immunity·R McCabeB Mullins
Sep 1, 1990·Antimicrobial Agents and Chemotherapy·M Gonzales-PerdomoS Goldenberg
Oct 1, 1982·Analytical Biochemistry·L C GreenS R Tannenbaum
Nov 1, 1994·Infection and Immunity·G N VespaJ S Silva
Dec 1, 1995·Infection and Immunity·J S SilvaF Q Cunha
Jan 11, 2000·Circulation·F S MachadoJ S Silva
Jan 29, 2002·International Journal for Parasitology·Wenda Gao, Miercio A Pereira
May 7, 2002·Memórias do Instituto Oswaldo Cruz·José Rodriques Coura, Solange L de Castro
Aug 29, 2002·The Journal of Infectious Diseases·Alvaro J RomanhaRicardo T Gazzinelli
Nov 25, 2003·Parasitology Research·Wanderson D DaRochaSantuza M R Teixeira
Jul 13, 2004·Trends in Parasitology·Gonzalo PeluffoRafael Radi
Nov 16, 2004·Archives of Biochemistry and Biophysics·María Noel AlvarezRafael Radi
Apr 11, 2006·Journal of Leukocyte Biology·Rui Appelberg
Jun 24, 2006·Drug Discovery Today·Brian K Shoichet
Aug 22, 2007·European Journal of Medicinal Chemistry·Anayive Pérez-RebolledoHeloisa Beraldo
Jan 28, 2009·Acta Crystallographica. Section D, Biological Crystallography·Anthony L Spek
Jul 30, 2009·Journal of Medicinal Chemistry·Rafaela S FerreiraAdam R Renslo
Mar 18, 2010·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Carolina Paola KnubelClaudia Cristina Motrán
Apr 7, 2010·European Journal of Medicinal Chemistry·Claudia RodriguesHeloisa Beraldo
Oct 22, 2010·Bioorganic & Medicinal Chemistry·Marcelo Zaldini HernandesJames Hobson McKerrow
Jun 11, 2011·Advances in Experimental Medicine and Biology·Mohammed SajidJames H McKerrow
Sep 3, 2013·Antioxidants & Redox Signaling·Claudia N Paiva, Marcelo T Bozza
Jan 24, 2014·Acta Pharmaceutica : a Quarterly Journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, Dealing with All Branches of Pharmacy and Allied Sciences·Katja CerpnjakFranc Vrečer
Feb 26, 2015·Antimicrobial Agents and Chemotherapy·Nayara Cristina FonsecaRafaela Salgado Ferreira
Apr 2, 2016·PLoS Neglected Tropical Diseases·Grazielle R GoesLeda Q Vieira
Aug 3, 2016·Infection and Immunity·Andréia BarrosoFabiana S Machado
Sep 29, 2018·PloS One·Raíssa Bernardes da SilvaAndré Luiz Pedrosa
Oct 31, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Tamires Cunha AlmeidaÂngelo de Fátima
Jul 10, 2019·European Journal of Medicinal Chemistry·Glaécia A N PereiraRafaela S Ferreira
Sep 10, 2019·F1000Research·Bennedikte Kollerup MadsenJacob Rosenberg