TY - JOUR
T1 - Synthesis and characterization of copper(II) complexes of pyridine-2-carboxamidrazones as potent antimalarial agents
AU - Gokhale, Nikhil H.
AU - Padhye, Subhash B.
AU - Billington, David C.
AU - Rathbone, Daniel L.
AU - Croft, Simon L.
AU - Kendrick, Howard D.
AU - Anson, Christopher E.
AU - Powell, Annie K.
PY - 2003/6/5
Y1 - 2003/6/5
N2 - Copper(II) complexes of some pyridine-2-carboxamidrazones have been prepared and characterized. The crystal structures of the copper complex cis-[dichloro(N1-2-acetylthiophene-pyridine-2-carboxamidrazone) copper(II)] 8a and one of the free ligands, viz. {(p-chloro-2-thioloxy-benzylidine-pyridine-2-carboxamidrazone)} 6, have been determined. The former shows a highly distorted square planar geometry around copper, with weak intermolecular coordination from the thiophenyl sulfur resulting in a stacking arrangement in the crystal lattice. The in vitro activities of the synthesized compounds against the malarial parasite Plasmodium falciparum are reported for the first time, which clearly shows the advantage of copper complexation and the requirement of four coordinate geometry around copper as some of the key structural features for designing such metal-based antimalarials. © 2003 Elsevier Science B.V. All rights reserved.
AB - Copper(II) complexes of some pyridine-2-carboxamidrazones have been prepared and characterized. The crystal structures of the copper complex cis-[dichloro(N1-2-acetylthiophene-pyridine-2-carboxamidrazone) copper(II)] 8a and one of the free ligands, viz. {(p-chloro-2-thioloxy-benzylidine-pyridine-2-carboxamidrazone)} 6, have been determined. The former shows a highly distorted square planar geometry around copper, with weak intermolecular coordination from the thiophenyl sulfur resulting in a stacking arrangement in the crystal lattice. The in vitro activities of the synthesized compounds against the malarial parasite Plasmodium falciparum are reported for the first time, which clearly shows the advantage of copper complexation and the requirement of four coordinate geometry around copper as some of the key structural features for designing such metal-based antimalarials. © 2003 Elsevier Science B.V. All rights reserved.
KW - antimalarial
KW - carboxamidrazones
KW - copper
KW - plasmodium falciparum
UR - http://www.scopus.com/inward/record.url?scp=0038730414&partnerID=8YFLogxK
UR - https://www.sciencedirect.com/science/article/pii/S0020169303000471?via%3Dihub
U2 - 10.1016/S0020-1693(03)00047-1
DO - 10.1016/S0020-1693(03)00047-1
M3 - Article
SN - 0020-1693
VL - 349
SP - 23
EP - 29
JO - Inorganica Chimica Acta
JF - Inorganica Chimica Acta
ER -