A natural product based DOS library of hybrid systems.
Eur J Med Chem
; 95: 41-8, 2015 May 05.
Article
em En
| MEDLINE
| ID: mdl-25794788
ABSTRACT
Here we described a natural product inspired modular DOS strategy for the synthesis of a library of hybrid systems that are structurally and stereochemically disparate. The main scaffold is a pyrroloisoquinoline motif, that is synthesized from tandem Pictet-Spengler lactamization. The structural diversity is generated via "privileged scaffolds" that are attached at the appropriate site of the motif. Screening of the library compounds for their antiplasmodial activity against chloroquine sensitive 3D7 cells indicated few compounds with moderate activity (20-50 µM). A systematic comparison of structural intricacy between the library members and a natural product dataset obtained from ZINC(®) revealed comparable complexity.
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Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Plasmodium falciparum
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Produtos Biológicos
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Eritrócitos
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Bibliotecas de Moléculas Pequenas
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Malária
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Antimaláricos
Limite:
Humans
Idioma:
En
Revista:
Eur J Med Chem
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
Índia