Anti-inflammation and antimalarial profile of 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester as a low molecular intermediate for hybrid drug synthesis

A novel 1,2,4-triazole intermediate 5-pyridin-2-yl-1H-[1,2,4]triazole-3-carboxylic acid ethyl ester was prepared by the reaction of N’-aminopiridyne-2-carboximidamine and an excess monoethyl oxalyl chloride and screened for biological activities. The compound was structurally characterized by nuclear magnetic resonance spectroscopy, elemental analysis, infrared spectroscopy, and single-crystal X-ray diffraction. Bioassays indicated that the compound exhibits potent anti-inflammation activity in vitro. An egg albumin denaturation assay to assess the anti-inflammatory effect of the synthesized compound showed a significant inhibition of protein with a maximum inhibition of 71.1% at the highest tested concentration (1000 µg/mL) compared to 81.3% for Aspirin as standard drug. The antimalarial activity on the 3D7 P. falciparum strain was determined to be IC50 176 µM and was obtained prior to connection with pharmacophoric groups

Eco-friendly synthesis, characterization, in vitro and in vivo anti-inflammatory activity of silver nanoparticle-mediated Selaginella myosurus aqueous extract

Introduction: There is emerging interest in medicinal plants in the biomedical field, due to their multitude of chemicals which show anti-inflammatory, antimicrobial, antiviral, or antitumoral potential. Research on medicinal plants has shown that nanotechnology could offer new solutions in the quality control, delivery aspects, or in sustaining herbal biological activities. This work reports on the preparation and characterization of silver nanoparticle-mediated Selaginella myosurus plant extract. Methods: Ultraviolet-visible spectroscopy, Fourier transform infrared spectroscopy, powder X-ray diffraction, energy dispersive X-ray spectroscopy, high-resolution scanning electron microscopy, high-resolution transmission electron microscopy, and selected area electron diffraction have been used to characterize the prepared silver nanoparticles. The synthetic stability was studied by varying concentrations and pH of reactants. Egg albumin denaturation and carrageenan-induced rat paw edema model were used to ascertain the anti-inflammation. Results: Ultraviolet-visible spectroscopy gave plasmon resonance ranging between 420 and 480 nm while Fourier transform infrared spectroscopy proved nano interface functionalized with organics. The powder X-ray diffraction pattern is in agreement with silver and silver chloride nanoparticles of crystallite size 33.7 nm and 44.2 nm for silver and silver chloride, respectively. Energy dispersive X-ray spectroscopy enables elemental characterization of the particles consisting of silver and silver chloride among main elements. Spherical silver grain of 58.81 nm average size has been depicted with high-resolution scanning electron microscopy and high-resolution transmission electron microscopy. Inhibitions of 99% and 60% were obtained in vitro and in vivo, respectively. Conclusion: The albumin denaturation and carrageenan-induced rat hind paw edema model to assess the anti-inflammatory potential of generated nanoparticles suggests that the silver nanoparticles may act as reducing/inhibiting agents on the release of acute inflammatory mediators. Hence, this work clearly demonstrated that silver nanoparticles mediated-Selaginella myosurus could be considered as a potential source for anti-inflammatory drugs

Natural Substances for the Synthesis of Silver Nanoparticles against Escherichia coli

The development of drug-resistant strains is rising and the search for new and novel ways of fighting new or reemerging microbes goes on. A hope of treating such multidrug-resistant infections came from plants mediated nanoparticles since nature is a generous source which provides a variety of chemical compounds that can be used for new drug discovery. Silver nanoparticles are reported to possess antiviral, antibacterial, antifungal, antiparasitic, larvicidal activity and anticancer properties. We reported green synthesis of silver nanoparticles mediated food plants Megaphrynium macrostachyum, Corchorus olitorus, Ricinodendron heudelotii, Gnetum bucholzianum, and Ipomoea batatas and their antibacterial efficacy against the Enterobacteriaceae Escherichia coli. The nature and size of the obtained nanoparticles are discussed as well as their Minimum Inhibitory Concentration (MIC) and the Minimum Bactericide Concentration (MBC) values considering their application in medical industry

Perspective: COVID-19 Outbreak and Information Tools

In April 2020, a novel coronavirus (COVID-19) outbreak originating in Wuhan, China, began spreading worldwide. There are currently more than two million cases. The World Health Organization has declared the viral spread to be a pandemic. The virus is transmitted between humans via droplets in the air and contaminated surfaces. After 2–14 days of incubation time, mild to severe symptoms occur, sometimes resulting in death. Key strategies for managing the pandemic are early detection, quarantine, and treatment. Many drugs or drug combinations like Hydroxychloroquine/Azithromycin or antiviruses like Remdesivir, which were originally designed to treat the Ebola virus, have been screened clinically to treat COVID-19 patients. Vaccines are likewise being developed by biotechnology companies and universities. We report in this paper how technology, and geographic information tools, can be used to control the pandemic in African settings. Different thematic such as flights tracking, electronic surveillance using web mass tools, temperature detectors, and telemedicine but also issues are developed.</p

Magnetic superexchange interactions: Trinuclear bis(oxamidato) versus bis(oxamato) type complexes

The diethyl ester of o-phenylenebis(oxamic acid) (opbaH2Et2) was treated with an excess of RNH2 in MeOH to cause the exclusive formation of the respective o-phenylenebis(N(R)-oxamides) (opboH4R2, R = Me 1, Et 2, nPr 3) in good yields. Treatment of 1–3 with half an equivalent of [Cu2(AcO)4(H2O)2] or one equivalent of [Ni(AcO)2(H2O)4] followed by the addition of four equivalents of [nBu4N]OH resulted in the formation of mononuclear bis(oxamidato) type complexes [nBu4N]2[M(opboR2)] (M = Ni, R = Me 4, Et 5, nPr 6; M = Cu, R = Me 7, Et 8, nPr 9). By addition of two equivalents of [Cu(pmdta)(NO3)2] to MeCN solutions of 7–9, novel trinuclear complexes [Cu3(opboR2)(L)2](NO3)2 (L = pmdta, R = Me 10, Et 11, nPr 12) could be obtained. Compounds 4–12 have been characterized by elemental analysis and NMR/IR spectroscopy. Furthermore, the solid state structures of 4–10 and 12 have been determined by single-crystal X-ray diffraction studies. By controlled cocrystallization, diamagnetically diluted 8 and 9 (1%) in the host lattice of 5 and 6 (99%) (8@5 and 9@6), respectively, in the form of single crystals have been made available, allowing single crystal ESR studies to extract all components of the g-factor and the tensors of onsite CuA and transferred NA hyperfine (HF) interaction. From these studies, the spin density distribution of the [Cu(opboEt2)]2− and [Cu(opbonPr2)]2− complex fragments of 8 and 9, respectively, could be determined. Additionally, as a single crystal ENDOR measurement of 8@5 revealed the individual HF tensors of the N donor atoms to be unequal, individual estimates of the spin densities on each N donor atom were made. The magnetic properties of 10–12 were studied by susceptibility measurements versus temperature to give J values varying from −96 cm−1 (10) over −104 cm−1 (11) to −132 cm−1 (12). These three trinuclear CuII-containing bis(oxamidato) type complexes exhibit J values which are comparable to and slightly larger in magnitude than those of related bis(oxamato) type complexes. In a summarizing discussion involving experimentally obtained ESR results (spin density distribution) of 8 and 9, the geometries of the terminal [Cu(pmdta)]2+ fragments of 12 determined by crystallographic studies, together with accompanying quantum chemical calculations, an approach is derived to explain these phenomena and to conclude if the spin density distribution of mononuclear bis(oxamato)/bis(oxamidato) type complexes could be a measure of the J couplings of corresponding trinuclear complexes