Letters in Drug Design & Discovery

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


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.


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

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