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A natural product based DOS library of hybrid systems
Ganesh Prabhu1, Shalini Agarwal2, Vijeta Sharma3
1Department of Chemistry, Shiv Nadar University, Post Office Shiv Nadar University, Pin 201314, Uttar Pradesh, India.
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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