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A natural product based DOS library of hybrid systems.
Prabhu, Ganesh; Agarwal, Shalini; Sharma, Vijeta; Madurkar, Sanjay M; Munshi, Parthapratim; Singh, Shailja; Sen, Subhabrata.
Afiliação
  • Prabhu G; Department of Chemistry, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India.
  • Agarwal S; International Center for Genetic Engineering and Biotechnology, Aruna Asaf Ali Marg, Pin 110067, New Delhi, India.
  • Sharma V; Department of Life Science, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India.
  • Madurkar SM; Department of Chemistry, Mahatma Gandhi University, Pin 793101, Meghalaya, India.
  • Munshi P; Department of Chemistry, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India.
  • Singh S; Department of Life Science, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India. Electronic address: shailja.singh@snu.edu.in.
  • Sen S; Department of Chemistry, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India. Electronic address: subhabrata.sen@snu.edu.in.
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 / Produtos Biológicos / Eritrócitos / Bibliotecas de Moléculas Pequenas / Malária / Antimaláricos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Índia

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Plasmodium falciparum / Produtos Biológicos / Eritrócitos / Bibliotecas de Moléculas Pequenas / Malária / Antimaláricos Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2015 Tipo de documento: Article País de afiliação: Índia