A Fragmenting Hybrid Approach for Targeted Delivery of Multiple Therapeutic Agents to the Malaria Parasite | Zendy

Mahajan Sumit S. | Zendy; Deu Edgar | Zendy; Lauterwasser Erica M. W. | Zendy; Leyva Melissa J. | Zendy; Ellman Jonathan A. | Zendy; Bogyo Matthew | Zendy; Renslo Adam R. | Zendy

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A Fragmenting Hybrid Approach for Targeted Delivery of Multiple Therapeutic Agents to the Malaria Parasite

Author(s) -

Mahajan Sumit S.,

Deu Edgar,

Lauterwasser Erica M. W.,

Leyva Melissa J.,

Ellman Jonathan A.,

Bogyo Matthew,

Renslo Adam R.

Publication year - 2011

Publication title -

chemmedchem

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.817

H-Index - 100

eISSN - 1860-7187

pISSN - 1860-7179

DOI - 10.1002/cmdc.201100002

Subject(s) - artemisinin , malaria , combinatorial chemistry , drug , plasmodium falciparum , pharmacology , drug delivery , malaria vaccine , drug resistance , chemistry , biology , immunology , microbiology and biotechnology , organic chemistry

Hybrid drugs with a twist: The coupling of iron(II)‐promoted trioxolane ring scission with a β‐elimination reaction enables the targeted delivery of multiple drug activities to the malaria parasite. A prototypical fragmenting hybrid (shown) comprises an iron(II)‐reactive 1,2,4‐trioxolane ring (red) joined via a masked retro‐Michael linker (blue) to a partner drug—in this case a protease inhibitor (green). Successful delivery of the protease inhibitor to intra‐erythrocytic Plasmodium falciparum parasites is demonstrated using a chemical–biological approach.

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