Thiopurine derivatives containing triazole and steroid: synthesis, antimalarial and antileishmanial activities.
A series of novel 6-thiopurine derivates containing 1,2,3-triazole were synthesized and their in vivo antimalarial activity and in vitro antileishmanial activity were examined. The compounds 10, 11, 12 and 14 presented higher values of inhibition of parasite multiplication than chloroquine. For antileishmanial activity, the compound 14 showed activity against the three species of Leishmania tested. None of compounds showed cytotoxicity against mammalian cells.
Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Campus Universitário, Juiz de Fora, Minas Gerais 36036-900, Brazil.
Roberta C N R
RC
Corrales
Nicolli B
NB
de Souza
Liliane S
LS
Pinheiro
Clarice
C
Abramo
Elaine S
ES
Coimbra
Adilson David
AD
Da Silva
D019342:Acetic Acid / Q000737:chemistry; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002738:Chloroquine / Q000737:chemistry; D005260:Female; D007891:Leishmania / Q000187:drug effects*; D015122:Mercaptopurine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D010961:Plasmodium / Q000187:drug effects*; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D000981:Antiprotozoal Agents; D013256:Steroids; D014230:Triazoles; D002738:Chloroquine; D015122:Mercaptopurine; D019342:Acetic Acid