Leishmanicidal activity of new megazol derivatives.
A series of thirteen new megazol derivatives, designed exploring the molecular hybridization approach between megazol (3) and heterocombretastatins (2), was synthesized. These new compounds were tested for in vitro antiparasitic activity upon axenic amastigotes of Leishmania donovani. Biological results led us to identify a new potent megazol derivative (4g), which presents an IC(50) = 0.081microg/mL, more active tham the reference drug miltefosine (IC(50) = 0.131microg/mL).
Riente
R R
RR
FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos - Far Manguinhos Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
Souza
V P
VP
Carvalho
S A
SA
Kaiser
M
M
Brun
R
R
da Silva
E F
EF
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001632:Bibenzyls / Q000737:chemistry; D002460:Cell Line; D015195:Drug Design; D020128:Inhibitory Concentration 50; D007891:Leishmania / Q000187:drug effects*; D051381:Rats; D013450:Sulfones / Q000737:chemistry; D013830:Thiadiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
D000981:Antiprotozoal Agents; D001632:Bibenzyls; D013450:Sulfones; D013830:Thiadiazoles; C013378:megazol; C040105:combretastatin