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Design and Synthesis of Endoperoxide Antimalarial Prodrug Models
Author(s) -
O'Neill Paul M.,
Stocks Paul A.,
Pugh Matthew D.,
Araujo Nuna C.,
Korshin Edward E.,
Bickley Jamie F.,
Ward Stephen A.,
Bray Patrick G.,
Pasini Erica,
Davies Jill,
Verissimo Edite,
Bachi Mario D.
Publication year - 2004
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200453859
Subject(s) - prodrug , bicyclic molecule , combinatorial chemistry , embedding , pharmacology , chemistry , computer science , medicine , stereochemistry , artificial intelligence
A masked combination chemotherapy which relies on the embedding of a number of active components, in a latent form, within a single endoperoxidic chemical entity is the aim of the research presented. The approach is illustrated by means of purposely designed bicyclic endoperoxide prodrug prototypes 1 and subsequently validated through the study of model compounds 2 (Ar=Ph, p ‐FC 6 H 4 , p ‐ClC 6 H 4 ).