PMID- 8676344
OWN - NLM
STAT- MEDLINE
DCOM- 19960815
LR  - 20131121
IS  - 0022-2623 (Print)
IS  - 0022-2623 (Linking)
VI  - 39
IP  - 5
DP  - 1996 Mar 1
TI  - Toward a novel metal-based chemotherapy against tropical diseases. 2. Synthesis 
      and antimalarial activity in vitro and in vivo of new ruthenium- and 
      rhodium-chloroquine complexes.
PG  - 1095-99
AB  - Chloroquine free base (CQ) reacts with [Rh(COD)Cl]2 (COD = 1,5-cyclooctadiene) 
      and RuCl3.-3H2O/Zn to yield Rh(COD)(CQ)Cl (1) and [RuCl2(CQ)]2 (2), respectively. 
      The two novel metal- CQ complexes, which were characterized mainly by 1D and 2D 
      NMR spectroscopy, were tested against Plasmodium berghei. The in vitro activity 
      of 1 was comparable to that of chloroquine diphosphate (CQDP), whereas 2 was 
      about 5 times more active. In in vivo tests at equivalent concentrations of free 
      CQ, CQDP reduced the parasitemia by 55%, while for complexes 1 and 2 the 
      reduction reached 73% and 94%, respectively, without any sign of acute toxicity 
      being observed up to 30 days after treatment. The Ru derivative 2 was further 
      evaluated against two chloroquine-resistant strains of Plasmodium falciparum, and 
      it was found to be 2-5 times more active than CQDP.
FAU - Sanchez-Delgado, R A
AU  - Sanchez-Delgado RA
AD  - Transition Metal Chemistry, Instituto Venezolano de Investigaciones Cientificas, 
      Caracas, Venezuela.
FAU - Navarro, M
AU  - Navarro M
FAU - Perez, H
AU  - Perez H
FAU - Urbina, J A
AU  - Urbina JA
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - J Med Chem
JT  - Journal of medicinal chemistry
JID - 9716531
RN  - 0 (Antimalarials)
RN  - 0 (Organometallic Compounds)
RN  - 0 (bis(ruthenium(chloroquine)dichloride))
RN  - 0 (rhodium(1,5-cyclooctadiene)(chloroquine)chloride)
RN  - 886U3H6UFF (Chloroquine)
SB  - IM
MH  - Animals
MH  - Antimalarials/*chemical synthesis/pharmacology/therapeutic use
MH  - Chloroquine
MH  - Drug Resistance
MH  - Female
MH  - Magnetic Resonance Spectroscopy
MH  - Malaria/*drug therapy
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Molecular Structure
MH  - Organometallic Compounds/*chemical synthesis/pharmacology/therapeutic use
MH  - Plasmodium berghei/*drug effects
MH  - Plasmodium falciparum/*drug effects
EDAT- 1996/03/01 00:00
MHDA- 1996/03/01 00:01
CRDT- 1996/03/01 00:00
PHST- 1996/03/01 00:00 [pubmed]
PHST- 1996/03/01 00:01 [medline]
PHST- 1996/03/01 00:00 [entrez]
AID - jm950729w [pii]
AID - 10.1021/jm950729w [doi]
PST - ppublish
SO  - J Med Chem. 1996 Mar 1;39(5):1095-99. doi: 10.1021/jm950729w.