Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites |
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Authors: | Tyrell Towle Isabel Chang Robert J. Kerns Purnima Bhanot |
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Affiliation: | 1. Division of Medicinal and Natural Products Chemistry, Department of Pharmaceutical Sciences and Experimental Therapeutics, College of Pharmacy, The University of Iowa, 115 S. Grand Ave., S311 PHAR, Iowa City, IA 52240, USA;2. Department of Microbiology and Molecular Genetics, University of Medicine and Dentistry of New Jersey, New Jersey Medical School, Newark, NJ 07103, USA |
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Abstract: | Malaria is a disease that has a major impact in many developing nations, especially on the African continent. There is a need to develop new therapeutics and prophylactic treatments against it. A trisubstituted pyrrole was recently found to inhibit infection of mammalian hepatocytes by Plasmodium sporozoites, but the target of this agent is not known. In this study trisubstituted pyrrole derivatives with different substituents on a piperidinyl nitrogen were prepared. We determined if modifications of the piperidinyl nitrogen would accommodate a drug–biotin linking strategy for affinity purification of the trisubstituted pyrrole’s target protein(s). |
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