Letters in Drug Design & Discovery

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

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Synthesis and In Vivo Antimalarial Activity of Novel Derivatives of 6- Mercaptopurine

Author(s): Roberta Reis Soares, Roberta C. N. R. Corrales, Fernanda Valerio Lopes, Marcio Jose M. Alves, Adilson David Da Silva, Clarice Abramo.

Abstract:

Chloroquine has been widely used to treat malaria, however, it is currently largely ineffective due to widespread parasite resistance. In this work, five 6-mercaptopurine derivates were synthesized and their in vivo antimalarial activity was examined. Among the three derivates of 6-mercaptopurine containing 1,2,3-triazole, compound 16 stands out, which showed increased activity over the days analyzed, inhibiting the growth of parasites in a way similar or even superior to chloroquine. Also, among the derivates of 6-mercaptopurine containing steroid, the analog 18 exhibited suppression of parasitaemia close to that of chloroquine. None of compounds showed cytotoxicity against mammalian cells.

Keywords: Antimalarial activities, Chemotherapy, Click chemistry, STEROIDS, 6-thiopurine, 1, 2, 3-triazole.

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Article Details

VOLUME: 10
ISSUE: 8
Year: 2013
Page: [741 - 747]
Pages: 7
DOI: 10.2174/15701808113109990017
Price: $58