Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library

Carolyn Dilanni Carroll, Hitesh Patel, Theodore O. Johnson, Tao Guo, Marc Orlowski, Zhen Min He, Cullen L. Cavallaro, Joan Guo, Anna Oksman, Ilya Y. Gluzman, James Connelly, Daniel Chelsky, Daniel E. Goldberg, Roland E. Dolle

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82 Scopus citations

Abstract

An encoded 13,020-member combinatorial library was synthesized containing a statine core. Evaluation of this library with plasmepsin II, an aspartyl protease required for hemoglobin metabolism in the malaria parasite, led to the identification of potent and selective inhibitors as well as novel structure-activity relationships.

Original languageEnglish
Pages (from-to)2315-2320
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume8
Issue number17
DOIs
StatePublished - Sep 8 1998
Externally publishedYes

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    Carroll, C. D., Patel, H., Johnson, T. O., Guo, T., Orlowski, M., He, Z. M., Cavallaro, C. L., Guo, J., Oksman, A., Gluzman, I. Y., Connelly, J., Chelsky, D., Goldberg, D. E., & Dolle, R. E. (1998). Identification of potent inhibitors of Plasmodium falciparum plasmepsin II from an encoded statine combinatorial library. Bioorganic and Medicinal Chemistry Letters, 8(17), 2315-2320. https://doi.org/10.1016/S0960-894X(98)00419-3