Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Synthesis and In Vivo Antimalarial Activity of Quinoline/Mercaptopurine Conjugates

Author(s): Nicolli Bellotti de Souza, Rafael Carvalhaes, Arturene Maria Lino do Carmo, Marcio Jose Martins Alves, Elaine Soares Coimbra, Sonia Maria Neumann Cupolilo, Clarice Abramo, Adilson David Da Silva.


In this paper we describe the preparation, characterization and antimalarial activity in vivo of novel quinoline/mercatopurine conjugates. The compounds were tested in vivo in a murine model using chloroquine as a reference compound. The values of inhibition of parasite multiplication relative to chloroquine were determined and the compound 4-(6’-mercatopurine)-7-chloroquinoline was considered statistically identical to chloroquine at the same dosage. The compounds were not cytotoxic at the maximum concentration used (100 μg/mL). Possible mechanisms of action are discussed. In light of these data, the title compounds may serve as prototypes for the development of novel antimalarial agents.

Keywords: Synthesis, Antimalarial activity, Plasmodium berghei, Quinoline, Chloroquine, Mercaptopurine, Anopheles mosquitoes, P. Falciparum, Plasmodium strains, de novo drug design, chemical modification, Thiopurines, immunosupressors, 6-mercaptopurine derivates, HRMS ESI

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Article Details

Year: 2012
Page: [361 - 366]
Pages: 6
DOI: 10.2174/157018012799859990
Price: $58