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Med Chem ; 5(4): 392-7, 2009 Jul.
Article in English | MEDLINE | ID: mdl-19689398

ABSTRACT

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).


Subject(s)
Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Leishmania/drug effects , Thiadiazoles/chemistry , Thiadiazoles/pharmacology , Animals , Antiprotozoal Agents/chemical synthesis , Antiprotozoal Agents/toxicity , Bibenzyls/chemistry , Cell Line , Drug Design , Inhibitory Concentration 50 , Rats , Sulfones/chemistry , Thiadiazoles/chemical synthesis , Thiadiazoles/toxicity
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