期刊
JOURNAL OF INORGANIC BIOCHEMISTRY
卷 105, 期 7, 页码 985-990出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2011.03.019
关键词
Bioorganometallic chemistry; Chromium; Antimalarial; Chloroquine
资金
- Swedish International Development Cooperation Agency (SIDA)
- Swedish Research Council (VR)
- SIDA/NRF
Organometallic analogs of chloroquine (CQ) are of interest as drug candidates that may be able to overcome the widespread chloroquine resistance developed by malaria parasites. Two new chromium arene CQ-analogs: [eta(6)-N-(7-chloroquinolin-4-yl)-N'-(2-dimethylamino-methylbenzyl)-ethane-1,2-diamine]tricarbonylchromium 4 and [eta(6)-N-(7-chloroquinolin-4-yl)-N'-(2-dimethylaminobenzyl)-ethane-1,2-diamine]tricarbonylchromium 9 have been synthesized and characterized. In addition, X-ray crystal structures of the intermediates (eta(6)-benzyldimethylamine)tricarbonylchromium 2, [eta(6)-2-((dimethylamino)methyl) benzaldehyde]tricarbonylchromium 3 and p-(eta(6)-dimethylaminobenzaldehyde)tricarbonyl chromium 8 are reported. Compound 4 was more active than chloroquine against both CQ-sensitive and CQ-resistant strains of Plasmodium falciparum when antimalarial activity was tested in vitro. The activity of 4 against the CQ-resistant parasite strain was twice as high as for the organic ligand alone (IC50 values of 33.9 nM versus 63.1 nM). (C) 2011 Published by Elsevier Inc.
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