Nonbisphosphonate inhibitors of Plasmodium falciparum FPPS/GGPPS.
Bioorg Med Chem Lett
; 41: 127978, 2021 06 01.
Article
em En
| MEDLINE
| ID: mdl-33766764
ABSTRACT
A series of novel thiazole-containing amides were synthesized. A structure-activity relationship study of these compounds led to the identification of potent and selective PfFPPS/GGPPS inhibitors with good in vitro ADME profiles. The most promising candidate molecules were progressed to mouse in vivo PK studies and demonstrated adequate free drug exposure to warrant further investigation.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
/
Difosfonatos
/
Inibidores Enzimáticos
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Farnesiltranstransferase
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Geraniltranstransferase
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Antimaláricos
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article