Coordination Compounds as Antivirals against Neglected Tropical Diseases.

Neglected tropical viral diseases are a burden to social and economic welfare being responsible for higher pathogen-related mortality rates and chronic debilitating patient conditions. Climatic changes have widened up the infectibility ratio of such diseases, with autochthonous transmission in formerly temperate-to-cold environments. The slow-paced development of potential vaccines followed by the inexistence of antiviral drugs for such diseases considerably worsens the situation.

Triphenylphosphine gold(I) derivatives promote antiviral effects against the Chikungunya virus.

Herein a systematic series of four [AuLL']n+ n = 0, +1 complexes, where L = 1,3-bis(mesityl)imidazole-2-ylidene (IMes), or triphenylphosphine (PPh3), and L' = chloride, or 4-dimethylaminopyridine (DMAP), had their in vitro antiviral activity assessed against Chikungunya virus (CHIKV). The PPh3 derivatives inhibited viral replication by 99%, whereas the IMes derivatives about 50%. The lipophilicity of the PPh3 derivatives is higher than the IMes-bearing compounds, which can be related to their more prominent antiviral activities.

Investigating the antiproliferative activities of new Cu complexes with pyridine hydrazone derivatives of nalidixic acid.

To further explore the structural features and potential antibacterial and antitumor activities of polynuclear Cu coordination compounds with nalidixic acid (nx) derivatives, new complexes bearing nx hydrazones with N-pyridinyl moieties substituted at positions 2 and 3 (h2py and h3py) were synthesized. Complexes [Cu(CHNO)(CHNO)(HO)]4BF∙HO (1), and [Cu(CHNO)(CHNO)(HO)]4BF∙3HO (%) (2) were synthesized using h2py and h3py with Cu(BF)∙nHO as precursor, whereas the [Cu(CHNO)Cl]∙0.5HO complex (3) was synthesized with h2py and CuCl∙2HO.

Repurposing potential of rimantadine hydrochloride and development of a promising platinum(II)-rimantadine metallodrug for the treatment of Chikungunya virus infection.

Most of the patients infected with Chikungunya virus (CHIKV) develop chronic manifestations characterized by pain and deformity in joints, impacting their quality of life. The aminoadamantanes, in their turn, have been exploited due to their biological activities, with amantadine and memantine recently described with anti-CHIKV activities. Here we evaluated the antiviral activity of rimantadine hydrochloride (rtdH), a well-known antiviral agent against influenza A, its platinum complex (Pt-rtd), and the precursor cis-[PtCl(dmso)], against CHIKV infection in vitro.

Memantine hydrochloride: a drug to be repurposed against Chikungunya virus?

Background: Chikungunya fever is an endemic disease caused by the Chikungunya virus (CHIKV) to which there is no vaccine or effective antiviral drug treatment so far. Our study aimed to evaluate the potential anti-CHIKV activity of memantine hydrochloride (mtnH), a drug from the class of the aminoadamantanes approved for the treatment of Alzheimer´s disease, as a possible drug to be repurposed to the treatment of Chikungunya fever.

Methods: MtnH antiviral activity against CHIKV was determined by infecting BHK-21 cells with CHIKV-nanoluc, a virus carrying the marker nanoluciferase reporter, in the presence or absence of mtnH at concentrations ranging from 500 to 1.

What is holding back the development of antiviral metallodrugs? A literature overview and implications for SARS-CoV-2 therapeutics and future viral outbreaks.

In light of the Covid-19 outbreak, this review brings together historical and current literature efforts towards the development of antiviral metallodrugs. Classical compounds such as CTC-96 and auranofin are discussed in depth, as pillars for future metallodrug development. From the recent literature, both cell-based results and biophysical assays against potential viral biomolecule targets are summarized here.

Antivirals Against Coronaviruses: Candidate Drugs for SARS-CoV-2 Treatment?

Coronaviruses (CoVs) are a group of viruses from the family that can infect humans and animals, causing mild to severe diseases. The ongoing pandemic of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) represents a global threat, urging the development of new therapeutic strategies. Here we present a selection of relevant compounds that have been described from 2005 until now as having and/or antiviral activities against human and/or animal CoVs.

Functional protein nanostructures: a chemical toolbox.

Nature has evolved an optimal synthetic factory in the form of translational and posttranslational processes by which millions of proteins with defined primary sequences and 3D structures can be built. Nature's toolkit gives rise to protein building blocks, which dictates their spatial arrangement to form functional protein nanostructures that serve a myriad of functions in cells, ranging from biocatalysis, formation of structural networks, and regulation of biochemical processes, to sensing. With the advent of chemical tools for site-selective protein modifications and recombinant engineering, there is a rapid development to develop and apply synthetic methods for creating structurally defined, functional protein nanostructures for a broad range of applications in the fields of catalysis, materials and biomedical sciences.

Crystal structure and theoretical studies of the keto-enol isomerism of N,N'-bis(salicylidene)-o-phenylenediamine (salophen).

The Schiff base N,N'-bis(salicylidene)-o-phenylenediamine (salophen) was prepared by the condensation of salicylaldehyde with o-phenylenediamine in ethanol solution. The compound was characterized by elemental analysis, infrared (IR), (1)H, (13)C and (1)H(15)N HMBC nuclear magnetic resonance (NMR) spectroscopic measurements, and also by X-ray diffraction. The tautomerism of salophen was also studied by calculations using density functional theory (DFT).