Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.
J Med Chem
; 55(20): 8879-90, 2012 Oct 25.
Article
em En
| MEDLINE
| ID: mdl-23035716
ABSTRACT
Design of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in Plasmodium falciparum , the most lethal species of parasites that cause malaria, is described. Chemistry-driven optimization of compound 1 from a focused NMT inhibitor library led to the identification of two early lead compounds 4 and 25, which showed good enzyme and cellular potency and excellent selectivity over human NMT. These molecules provide a valuable starting point for further development.
Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Plasmodium falciparum
/
Benzofuranos
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Aciltransferases
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Antimaláricos
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article