نتایج جستجو برای: trypanocidal activity

تعداد نتایج: 1134678  

2013
Jonathan W Choy Clifford Bryant Claudia M Calvet Patricia S Doyle Shamila S Gunatilleke Siegfried S F Leung Kenny K H Ang Steven Chen Jiri Gut Juan A Oses-Prieto Jonathan B Johnston Michelle R Arkin Alma L Burlingame Jack Taunton Matthew P Jacobson James M McKerrow Larissa M Podust Adam R Renslo

Inhibition of the Trypanosoma cruzi cysteine protease cruzain has been proposed as a therapeutic approach for the treatment of Chagas' disease. Among the best-studied cruzain inhibitors to date is the vinylsulfone K777 (1), which has proven effective in animal models of Chagas' disease. Recent structure-activity studies aimed at addressing potential liabilities of 1 have now produced analogues ...

Journal: :The Yale Journal of Biology and Medicine 1950
B. A. Rubin

With techniques and materials previously described5 a number of lactones (both naturally occurring and synthetic), and some related compounds, have been shown to have definite in vitro trypanocidal activity. It was further shown that these compounds have therapeutic effect in vivo. The concept that specific chemical substances can interfere with the action of a chemotherapeutic agent provides a...

Journal: :Infection and immunity 1995
K A Norris J E Schrimpf J L Flynn S M Morris

The generation of nitric oxide (NO) is largely responsible for the intracellular killing of Trypanosoma cruzi by activated macrophages. The present study was carried out to determine whether the production of NO by activated murine macrophages cultured in physiologic levels of arginine can be augmented by increasing the availability of arginine, the substrate for NO biosynthesis. Increased exog...

Journal: :International journal of antimicrobial agents 2008
Gilberto L Pardo Andreu Natalia M Inada Rolando F Pellón Maite L Docampo Mirta L Fascio Norma B D'Accorso Anibal E Vercesi

M, Tompkins LS, editors. Campylobacter jejuni: current status and future trends. Washington, DC: American Society for Microbiology; 1992. [2] Drlica K, Zhao X. Mutant selection window hypothesis updated. Clin Infect Dis 2007;44:681–8. [3] National Committee for Clinical Laboratory Standards. Performance standards for antimicrobial disk and dilution susceptibility tests for bacteria isolated fro...

Journal: :The Yale Journal of Biology and Medicine 1948
Benjamin Arnold Rubin

The method of testing the therapeutic action of drugs by injecting them into infected laboratory animals, although an indispensable procedure, is not entirely adequate if the object of the inquiry is to obtain information regarding small quantitative differences between related compounds and their mechanism of action. Does a drug, as such, act directly on the parasites or only after it has unde...

Journal: :Memorias do Instituto Oswaldo Cruz 2004
Miguel A Chena Silvia Elizondo-Jiménez Lorena Rodríguez-Páez Benjamín Nogueda-Torres Isabel Baeza-Ramírez Carlos Wong-Ramírez

N-allyl (NAOx) and N-propyl (NPOx) oxamates were designed as inhibitors of alpha-hydroxyacid dehydrogenase (HADH) isozyme II from Trypanosoma cruzi. The kinetic studies showed that NAOx and NPOx were competitive inhibitors of HADH-isozyme II (Ki = 72 microM, IC50 = 0.33 mM and 70 microM, IC50 = 0.32 mM, respectively). The attachment of the allylic and propylic chains to nitrogen of the competit...

Journal: :Journal of enzyme inhibition 1998
A Fournet A Inchausti G Yaluff A Rojas De Arias H Guinaudeau J Bruneton M A Breidenbach P A Karplus C H Faerman

Eleven bisbenzylisoquinoline (BBIQ) alkaloids were studied for in vitro trypanocidal activity against trypomastigote forms of the Y strain of Trypanosoma cruzi. The inhibitory activity of these compounds against trypanothione reductase (TR), a target enzyme for chemotherapy against Chagas disease, was also studied. Six BBIQ alkaloids (antioquine, cepharanthine, daphnoline, limacine, cycleanine ...

Journal: :Infection and immunity 1999
J C Aliberti F S Machado R T Gazzinelli M M Teixeira J S Silva

Trypanosoma cruzi replicates in nucleated cells and is susceptible to being killed by gamma interferon-activated macrophages through a mechanism dependent upon NO biosynthesis. In the present study, the role of platelet-activating factor (PAF) in the induction of NO synthesis and in the activation of the trypanocidal activity of macrophages was investigated. In vitro, PAF induced NO secretion b...

2015
Maria J. Pineda de las Infantas y Villatoro Juan D. Unciti-Broceta Rafael Contreras-Montoya Jose A. Garcia-Salcedo Miguel A. Gallo Mezo Asier Unciti-Broceta Juan J. Diaz-Mochon

A novel one-pot synthesis of tri-substituted purines and the discovery of purine analogues with trypanocidal activity are reported. The reaction is initiated by a metal-free oxidative coupling of primary alkoxides and diaminopyrimidines with Schiff base formation and subsequent annulation in the presence of large N,N-dimethylamides (e.g. N,N-dimethylpropanamide or larger). This synthetic route ...

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