Solid-phase synthesis and bioevaluation of Lupeol-based libraries as antimalarial agents
2002; Elsevier BV; Volume: 12; Issue: 20 Linguagem: Inglês
10.1016/s0960-894x(02)00623-6
ISSN1464-3405
AutoresThangavelu Srinivasan, Gaurav Kumar Srivastava, Ashish K. Pathak, Sanjay Batra, K. Raj, Kshipra Singh, S.K. Puri, Bijoy Kundu,
Tópico(s)Antimicrobial Peptides and Activities
ResumoThe 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.
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