Preparation of Half-Sandwich Osmium Complexes by Deprotonation of Aromatic and Pro-aromatic Acids with a Hexahydride Brønsted Base

2011 ◽  
Vol 30 (14) ◽  
pp. 3844-3852 ◽  
Author(s):  
Miguel A. Esteruelas ◽  
Jorge García-Raboso ◽  
Montserrat Oliván
2019 ◽  
Vol 48 (9) ◽  
pp. 3116-3131 ◽  
Author(s):  
Gabriele Albertin ◽  
Stefano Antoniutti ◽  
Jesús Castro ◽  
Francesca Sibilla

The preparation and reactivity of a series of half-sandwich pentamethylcyclopentadienyl complexes of osmium containing diazoalkane, alkene, dioxygen, vinylidene and allenylidene ligands are described.


2004 ◽  
Vol 2004 (1) ◽  
pp. 17-32 ◽  
Author(s):  
Manuel Jiménez-Tenorio ◽  
M. Carmen Puerta ◽  
Pedro Valerga

ChemInform ◽  
2004 ◽  
Vol 35 (14) ◽  
Author(s):  
Manuel Jimenz-Tenorio ◽  
M. Carmen Puerta ◽  
Pedro Valerga

2011 ◽  
Vol 30 (7) ◽  
pp. 1930-1941 ◽  
Author(s):  
Alba Collado ◽  
Miguel A. Esteruelas ◽  
Enrique Oñate

2020 ◽  
Author(s):  
Sofia Alexandra Milheiro ◽  
Joana Gonçalves ◽  
Ricardo Lopes ◽  
Margarida Madureira ◽  
Lis Lobo ◽  
...  

<p><a>A small library of “half-sandwich” cyclopentadienylruthenium(II) compounds of general formula [(</a>η<sup>5</sup>-C<sub>5</sub>R<sub>5</sub>)Ru(PPh<sub>3</sub>)(N-N)][PF<sub>6</sub>], a scaffold hitherto unfeatured in the toolbox of antiplasmodials, was screened for activity against the blood stage of CQ-sensitive 3D7-GFP, CQ-resistant Dd2 and artemisinin-resistant IPC5202 <i>Plasmodium falciparum</i> strains, and the liver stage of <i>P. berghei</i>. The best performing compounds displayed dual-stage activity, with single-digit nM IC<sub>50</sub> values against blood stage malaria parasites, nM activity against liver stage parasites, and residual cytotoxicity against mammalian cells (HepG2, Huh7). Parasitic absorption/distribution of 7-nitrobenzoxadiazole-appended fluorescent compounds <b>Ru4</b> and <b>Ru5</b> was investigated by confocal fluorescence microscopy, revealing parasite-selective absorption in infected erythrocytes and nuclear accumulation of both compounds. The lead compound <b>Ru2</b> impaired asexual parasite differentiation, exhibiting fast parasiticidal activity against both ring and trophozoite stages of a synchronized <i>P. falciparum</i> 3D7 strain. These results point to cyclopentadienylruthenium(II) complexes as a highly promising chemotype for the development of dual-stage antiplasmodials.</p>


1992 ◽  
Vol 57 (5) ◽  
pp. 1134-1142 ◽  
Author(s):  
Bohuslav Rittich ◽  
Marta Pirochtová ◽  
Jiří Hřib ◽  
Kamila Jurtíková ◽  
Petr Doležal

The present paper deals with the relationship between biological activities of some aliphatic and aromatic acids and their physico-chemical parameters expressing the influence of hydrophobic factors. The test strain in the biotest of growth inhibition was the fungus Fusarium moniliforme CCMF-180 and Penicillium expansum CCMF-576. Significant relationship between antifungal activities of un-ionized form of aliphatic acids and their capacity factors (log k'0) extrapolated to pure water, partition coefficients determined in 1-octanol-water system (log Poct) and the first order of molecular connectivity indices (1χ) were calculated. The ionized form of aliphatic acids were antifungally active too. For benzoic acids significant relationships between antifungal activities and capacity factors of anionic form (log k'ia) were calculated.


2019 ◽  
Vol 38 (24) ◽  
pp. 4615-4624 ◽  
Author(s):  
Alexander N. Selikhov ◽  
Andrey S. Shavyrin ◽  
Anton V. Cherkasov ◽  
Georgy K. Fukin ◽  
Alexander A. Trifonov

Metallomics ◽  
2021 ◽  
Vol 13 (4) ◽  
Author(s):  
James P C Coverdale ◽  
Collette S Guy ◽  
Hannah E Bridgewater ◽  
Russell J Needham ◽  
Elizabeth Fullam ◽  
...  

Abstract The treatment of tuberculosis (TB) poses a major challenge as frontline therapeutic agents become increasingly ineffective with the emergence and spread of drug-resistant strains of Mycobacterium tuberculosis (Mtb). To combat this global health problem, new antitubercular agents with novel modes of action are needed. We have screened a close family of 17 organometallic half-sandwich Os(II) complexes [(arene)Os(phenyl-azo/imino-pyridine)(Cl/I)]+Y– containing various arenes (p-cymene, biphenyl, or terphenyl), and NMe2, F, Cl, or Br phenyl or pyridyl substituents, for activity towards Mtb in comparison with normal human lung cells (MRC5). In general, complexes with a monodentate iodido ligand were more potent than chlorido complexes, and the five most potent iodido complexes (MIC 1.25–2.5 µM) have an electron-donating Me2N or OH substituent on the phenyl ring. As expected, the counter anion Y (PF6–, Cl–, I–) had little effect on the activity. The pattern of potency of the complexes towards Mtb is similar to that towards human cells, perhaps because in both cases intracellular thiols are likely to be involved in their activation and their redox mechanism of action. The most active complex against Mtb is the p-cymene Os(II) NMe2-phenyl-azopyridine iodido complex (2), a relatively inert complex that also exhibits potent activity towards cancer cells. The uptake of Os from complex 2 by Mtb is rapid and peaks after 6 h, with temperature-dependence studies suggesting a major role for active transport. Significance to Metallomics Antimicrobial resistance is a global health problem. New advances are urgently needed in the discovery of new antibiotics with novel mechanisms of action. Half-sandwich organometallic complexes offer a versatile platform for drug design. We show that with an appropriate choice of the arene, an N,N-chelated ligand, and monodentate ligand, half-sandwich organo–osmium(II) complexes can exhibit potent activity towards Mycobacterium tuberculosis (Mtb), the leading cause of death from a single infectious agent. The patterns of activity of the 17 azo- and imino-pyridine complexes studied here towards Mtb and normal lung cells suggest a common redox mechanism of action involving intracellular thiols.


2021 ◽  
Author(s):  
János P. Mészáros ◽  
Veronika F. S. Pape ◽  
Gergely Szakács ◽  
Gábor Németi ◽  
Márk Dénes ◽  
...  

A series of half-sandwich polypyridyl complexes was synthesized and compared focusing on structural, cytotoxic and aqueous solution behaviour. The formula of the synthesized complexes is [M(arene)(N,N)Cl]Cl, where M: Ru or...


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