title: In vitro activities of thiadiazine derivatives against Leishmania amazonensis.
abstract: Ten thiadiazine derivatives were tested in vitro for antiparasitic effects against both extracellular promastigotes and intracellular amastigotes of Leishmania amazonensis. The results showed that the evaluated compounds exhibited a strong antiproliferative activity on all developmental stages of the parasite. The minimal inhibitory concentration and the 50 % effective concentration values against the promastigote were 2.1-5.1 microg/ml and 0.6-1.8 microg/ml, respectively. The tested compounds caused an irreversible inhibition of the promastigote growth either after 1 h of treatment with 10 microg/ml or after 24 h with 1 microg/ml. Also, the thiadiazine derivatives were active against amastigotes producing between 12 and 89 % of reduction of infection at 100 ng/ml. However, the compounds exhibited high toxicity and provoked inhibition of the phagocytosis in the murine host cell.
authors.affiliation: Departamento de Parasitologia, Instituto de Medicina Tropical "Pedro Kourí", Ciudad de la Habana (Cuba). monzote@ipk.sld.cu
authors.forename: Lianet
authors.initials: L
authors.lastname: Monzote
authors.forename: Ana M
authors.initials: AM
authors.lastname: Montalvo
authors.forename: Lisset
authors.initials: L
authors.lastname: Fonseca
authors.forename: Rolando
authors.initials: R
authors.lastname: Pérez
authors.forename: Margarita
authors.initials: M
authors.lastname: Suárez
authors.forename: Hortensia
authors.initials: H
authors.lastname: Rodríguez
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D005260:Female; D007894:Leishmania mexicana / Q000187:drug effects* / Q000254:growth & development; D008264:Macrophages / Q000187:drug effects / Q000469:parasitology; D008536:Meglumine / Q000494:pharmacology; D051379:Mice; D008807:Mice, Inbred BALB C; D010587:Phagocytosis / Q000187:drug effects; D013829:Thiadiazines / Q000494:pharmacology*
chemical_list: D000981:Antiprotozoal Agents; D013829:Thiadiazines; D008536:Meglumine