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Synthesis and in vitro/in vivo Evaluation of the Antitrypanosomal Activity of 3-Bromoacivicin, a Potent CTP Synthetase Inhibitor

The first convenient synthesis of enantiomerically pure (αS,5S)-α-amino-3-bromo-4,5-dihydroisoxazol-5-yl acetic acid (3-bromoacivicin) is described. We demonstrate that 3-bromoacivicin is a CTP synthetase inhibitor three times as potent as its 3-chloro analogue, the natural antibiotic acivicin. Beca...

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Detalles Bibliográficos
Autores principales: Conti, Paola, Pinto, Andrea, Wong, Pui E, Major, Louise L, Tamborini, Lucia, Iannuzzi, Maria C, De Micheli, Carlo, Barrett, Michael P, Smith, Terry K
Formato: Online Artículo Texto
Lenguaje:English
Publicado: WILEY-VCH Verlag 2011
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3504386/
https://www.ncbi.nlm.nih.gov/pubmed/21275056
http://dx.doi.org/10.1002/cmdc.201000417