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Abstract
A new ditopic, quinoline-based ligand L (7-chloro-4-(pyridin-4-yl)quinoline) was synthesized via a Suzuki cross-coupling reaction. The ligand was utilized to synthesize the corresponding half-sandwich iridium(III) and ruthenium(II) binuclear complexes (1c and 1d) and the subsequent metallarectangles (2c, 2d, 3c, and 3d), via [2 + 2] coordination-driven self-assembly. Single-crystal X-ray diffraction confirmed the proposed molecular structure of the binuclear complex [{IrCl2(Cp*)}2(μ-L)] (1c) and DFT calculations were used to predict the optimized geometry of the rectangular nature of [{Ir(μ-Cl)(Cp*)}4(μ-L)2](CF3SO3)4 (2c). All of the metallarectangles were isolated as their triflate salts and characterized using various spectroscopic (1H, 13C{1H}, DOSY NMR, and IR spectroscopy) and analytical techniques (ESI-MS). The synthesized compounds were screened against the NF54 chloroquine-sensitive (CQS) and K1 chloroquine-resistant (CQR) strains of Plasmodium falciparum. Incorporation of the ubiquitous quinoline core and metal complexation significantly enhanced the in vitro biological activity, with an increase in the nuclearity correlating with an increase in the resultant antiplasmodial activity. This was observed across both parasitic strains, alluding to the potential of supramolecular metallarectangles to act as antiplasmodial agents. Inhibition of haemozoin formation was considered a potential mechanism of action and selected metallarectangles exhibit β-haematin inhibition activity with near comparable activity to chloroquine.
Highlights
Malaria, an infectious mosquito-borne disease caused by a blood parasite of the genus Plasmodium, is associated with high levels of morbidity and mortality in adults and children and occurs throughout tropical and subtropical regions of the world.[1,2,3,4] Despite the overall number of estimated cases declining between 2010 to 2014, subsequent years have seen a resurgence in malaria cases globally.[1]
The quinoline scaffold continues to be attractive for the design and synthesis of new antimalarial agents
Thereafter, the addition of ligand L resulted in coordination at the vacant coordination sites, and the resultant complexes (3c and 3d) formed via coordinationdriven self-assembly
Summary
An infectious mosquito-borne disease caused by a blood parasite of the genus Plasmodium, is associated with high levels of morbidity and mortality in adults and children and occurs throughout tropical and subtropical regions of the world.[1,2,3,4] Despite the overall number of estimated cases declining between 2010 to 2014, subsequent years have seen a resurgence in malaria cases globally.[1] The World Health Organisation (WHO) estimated that in 2019 there were approximately 229 million cases of malaria worldwide.[1]. The eventual recognition of quinoline-based antimalarials, such as chloroquine (CQ),[5] provided new hope for the treatment of this disease. Cost-effective synthesis, ease of use, and excellent clinical efficiency[6] have
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