Comparing The Antileishmanial Activity Of Gold(I) And Gold(Iii) Compounds Inl. Amazonensisandl. Braziliensis In Vitro

: A series of mononuclear coordination or organometallic Au-I/Au(III)complexes (1-9) have been comparatively studiedin vitrofor their antileishmanial activity against promastigotes and amastigotes, the clinically relevant parasite form, ofLeishmania amazonensisandLeishmania braziliensis. One of the cationic Au(I)bis-N-heterocyclic carbenes (3) has low EC(50)values (ca. 4 mu M) in promastigotes cells and no toxicity in host macrophages. Together with two other Au(III)complexes (6and7), the compound is also extremely effective in intracellular amastigotes fromL. amazonensis. Initial mechanistic studies include an evaluation of the gold complexes ' effect onL. amazonensis'plasma membrane integrity.