A comparative study of mesoionic compounds in Leishmania sp. and toxicity evaluation.
In this first study, a series of mesoionic compounds like 1,3,4-thiadiazolium-2-phenylamine derivatives were synthesized and studied in Leishmania amazonensis. The cytotoxic effects of these compounds on the host cells were investigated and the antileishmanial in vitro activity was compared with other species of Leishmania (Leishmania chagasi and Leishmania braziliensis). The compounds presented lower toxicity in murine macrophages than the reference drug pentamidine. The halogen derivatives 5, 6, 8 and 13 (4-F, 4-Cl, 4-Br and 3-Cl) were the most active compounds among all the species tested.
Rodrigues
Raquel F
RF
Fundação Oswaldo Cruz, Departamento de Imunologia, IOC/FIOCRUZ, 21045-900 Rio de Janeiro, Brazil.
da Silva
Edson F
EF
Echevarria
Aurea
A
Fajardo-Bonin
Renata
R
Amaral
Veronica F
VF
Leon
Leonor L
LL
Canto-Cavalheiro
Marilene M
MM
D000818:Animals; D000981:Antiprotozoal Agents / Q000009:adverse effects / Q000494:pharmacology* / Q000633:toxicity*; D006863:Hydrogen-Ion Concentration; D007891:Leishmania / Q000737:chemistry* / Q000187:drug effects*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents