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.

Journal Name: Letters in Drug Design & Discovery

Volume 9 , Issue 4 , 2012

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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

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