2013
DOI: 10.1128/aac.01870-12
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In Vitro and In Vivo Activities of 2-Aminopyrazines and 2-Aminopyridines in Experimental Models of Human African Trypanosomiasis

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Cited by 11 publications
(7 citation statements)
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“…The traditional route to identify such therapeutic agents has been to search for compounds that will target genes or pathways necessary for cell viability. Indeed, whole-cell based high-throughput screening for trypanostatic and trypanocidal agents is well established (Hesse et al, 1995 ; Mackey et al, 2006 ; Sykes and Avery, 2009 ; Jones et al, 2010 ; De Rycker et al, 2012 ; Sykes et al, 2012 ; Vodnala et al, 2013 ) and multiple classes of compounds with potential for development into new therapeutics are being pursued (Mackey et al, 2006 ; Jones et al, 2010 ; Sykes et al, 2012 ; Vodnala et al, 2013 ). However, phenotypic screens for genes or pathways involved in the establishment, maintenance or transmission of infection could provide an alternative or complementary route to the identification of novel therapeutics with anti-virulence or transmission-blocking potential.…”
Section: Phenotypic Screening For Stumpy Formation Via Small Compoundmentioning
confidence: 99%
“…The traditional route to identify such therapeutic agents has been to search for compounds that will target genes or pathways necessary for cell viability. Indeed, whole-cell based high-throughput screening for trypanostatic and trypanocidal agents is well established (Hesse et al, 1995 ; Mackey et al, 2006 ; Sykes and Avery, 2009 ; Jones et al, 2010 ; De Rycker et al, 2012 ; Sykes et al, 2012 ; Vodnala et al, 2013 ) and multiple classes of compounds with potential for development into new therapeutics are being pursued (Mackey et al, 2006 ; Jones et al, 2010 ; Sykes et al, 2012 ; Vodnala et al, 2013 ). However, phenotypic screens for genes or pathways involved in the establishment, maintenance or transmission of infection could provide an alternative or complementary route to the identification of novel therapeutics with anti-virulence or transmission-blocking potential.…”
Section: Phenotypic Screening For Stumpy Formation Via Small Compoundmentioning
confidence: 99%
“…A screening of 5500 small molecules identified 2-aminopyrazines and 2-aminopyridines as hit structures. 57 Since the most effective compound 20 (Fig. 8) exhibited in vitro activity against Trypanosoma subsp.…”
Section: -Aminopyrazines/2-aminopyridinesmentioning
confidence: 99%
“…However, more detailed in vivo investigation about bioavailability and other preclinical properties is in progress. 57…”
Section: -Aminopyrazines/2-aminopyridinesmentioning
confidence: 99%
“…19 As a consequence, several approaches for the synthesis of pyrrolo [2,3-b]pyrazines have been developed [20][21][22][23] although more general and selective methods to prepare polysubtituted 4,7-diazaindoles would still be welcome. As a continuation of our studies on the utility of pyridinium N-heteroarylaminides 1 (Scheme 1) as suitable scaffolds [24][25][26][27] to obtain 2-aminoazines, [28][29][30] compounds that, in addition to other uses, have recently been tested in experimental models of human African trypanosomiasis, 31 we became interested in developing a synthetic route to pyrrolo [2,3-b]pyridines and pyrrolo [2,3-b]pyrazines starting from the corresponding N-pyridin-2-yl or pyrazin-2-yl pyridinium aminide (1a, 1b, Scheme 1). Pyridinium N-heteroarylaminides 1 are stable heterocyclic betaines in which the negative charge is stabilized by both the pyridinium and the azine moieties.…”
Section: Introductionmentioning
confidence: 96%