C. Biot et al., Synthesis and antimalarial activity in vitro of potential metabolites of ferrochloroquine and related compounds, BIO MED CH, 7(12), 1999, pp. 2843-2847
In man, the two major metabolites of the antimalarial drug chloroquine (CQ)
are monodesethylchloroquine (DECQ) and didesethylchloroquine (di-DECQ). By
analogy with CQ, the synthesis and the in vitro tests of some amino deriva
tives of ferrochloroquine (FQ), a ferrocenic analogue of CQ which are presu
med to be the oxidative metabolites of FQ, are reported. Desmethylferrochlo
roquine 1a and didesmethylferrochloroquine 2 would be more potent against s
chizontocides than CQ in vitro against two strains (HB3 and Dd2) of Plasmod
ium falciparum. Other secondary amino derivatives have been prepared and pr
oved to be active as antimalarial agents in vitro, too. (C) 1999 Published
by Elsevier Science Ltd. ALI rights reserved.