Pharmacopeia Inc.

Shiwei Tao

Roland Ellwood Dolle

Hitesh K Patel

Theodore Otto Johnson, Jr

Tao Guo

Zhen Min He

Carolyn DiIanni Carroll

Combination chemical libraries of Formula I

Combinatorial hydroxy-amino acid amide libraries

Combinatorial chemical libraries of Formula I ##STR1## and methods for their preparation are disclosed. The libraries allow one to screen large numbers of compounds for a desired biological activity with relative ease. The libraries may be tagged or untagged. In preferred libraries, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. The use of the libraries to discover biologically active compounds is also disclosed.

Compounds of Formula I ##STR1## are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.

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Plainsboro, NJ, United States of America

Shiwei Tao