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Solid-phase synthesis and bioevaluation of lupeol-based libraries as antimalarial agents.

Abstract：

:The use of the triterpenoid lupeol as a scaffold for the synthesis of lupeol-based libraries is described. Lupeol was anchored to a solid support (Rink amide/Sieber Amide) through aliphatic dicarboxylic acid moieties, which also served as a site for introducing diversity. The resulting polymer linked 3beta-O (resin-alkanoyl)-lup-20(29)-ene 3 was used to generate key intermediates 3beta-O (resin-alkanoyl)-30-bromo-lup-20(29)-ene 4 and 3beta-O (resin-alkanoyl)-30-amino-lup-20(29)-ene 6 for the generation of libraries based on disubstituted lupeol derivatives. A 96-member library was screened for its in-vitro antimalarial activity against Plasmodium falciparum.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Srinivasan T,Srivastava GK,Pathak A,Batra S,Raj K,Singh K,Puri SK,Kundu B

doi

10.1016/s0960-894x(02)00623-6

subject

Has Abstract

pub_date

2002-10-21 00:00:00

pages

2803-6

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960894X02006236

journal_volume

12

pub_type

杂志文章

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