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

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

Volume: 10 Issue: 8

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

Affiliation:

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

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.

Cite this article as:

Soares Reis Roberta, Corrales C. N. R. Roberta, Lopes Valerio Fernanda, Alves Jose M. Marcio, Silva David Da Adilson and Abramo Clarice, Synthesis and In Vivo Antimalarial Activity of Novel Derivatives of 6- Mercaptopurine, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113109990017