Pyrazolone-type compounds (part II): and evaluation of antioxidant potential; structure-activity relationship.

The pyrazolone class comprises a variety of hybrid compounds displaying diverse biological actions. Although studied for decades, these compounds are still of interest due to their facile chemical transformations. In our previous work, we presented the synthetic route of functionalised pyrazolone derivatives.

Pyrazolone-type compounds: synthesis and assessment of antiviral potential against key viral proteins of SARS-CoV-2.

Coronavirus outbreak is still a major public health concern. The high mutation ability of SARS-CoV-2 periodically delivers more transmissible and dangerous variants. Hence, the necessity for an efficient and inexpensive antiviral agent is urgent.

Pyrazole Derivatives of Medically Relevant Phenolic Acids: Insight into Antioxidative and Anti-LOX Activity.

Background: From the point of view of medicinal chemistry, compounds containing phenolic and pyrazolic moiety are significant since they are often constituents of bioactive compounds.

Objective: The aims of this study were to synthesize pyrazole derivatives of medically relevant phenolic acids, confirm their structure, and evaluate their antioxidative and anti-LOX activities.

Methods: Phenolic pyrazole derivatives were obtained, starting from esters of medically relevant phenolic acids.

A new efficient domino approach for the synthesis of pyrazolyl-phthalazine-diones. Antiradical activity of novel phenolic products.

Pyrazolyl-phthalazine-dione derivatives (PPDs) were synthetized in the ionic liquid catalyzed one-pot multicomponent reaction of acetylacetone, 2,3-dihydrophthalazine-1,4-dione, and different aldehydes in moderate to good yields. Six new PPDs were obtained, and the crystal structure of 2-acetyl-1-(4-fluorophenyl)-3-methyl-1-pyrazolo[1,2-]phthalazine-5,10-dione (PPD-4) was determined. The most interesting structural features of the novel PPD-4 is the formation of a rather short intermolecular distance between the F atom of one molecule and the midpoint of the neighbouring six-membered heterocyclic ring.

Investigation of the antioxidant and radical scavenging activities of some phenolic Schiff bases with different free radicals.

The antioxidant properties of some phenolic Schiff bases in the presence of different reactive particles such as (•)OH, (•)OOH, (CH2=CH-O-O(•)), and (-•)O2 were investigated. The thermodynamic values, ΔH BDE, ΔH IP, and ΔH PA, were used for this purpose. Three possible mechanisms for transfer of hydrogen atom, concerted proton-electron transfer (CPET), single electron transfer followed by proton transfer (SET-PT), and sequential proton loss electron transfer (SPLET) were considered.

Insight into hydrolytic reaction of N-acetylated L-histidylglycine dipeptide with novel mechlorethamine platinum(II) complex. NMR and DFT study of the hydrolytic reaction.

The reaction of K(2)PtCl(4) with the alkylating agent mechlorethamine hydrochloride, at a molar ratio of 1:2, results in the formation of 2-chloro-N-(2-chloroethyl)-N-methylethylammonium-tetrachloridoplatinate(II) complex. The hydrolytic activity of the novel Pt(II) complex was tested in the reaction with N-acetylated L-histidylglycine dipeptide at a molar ratio 1:1. It was shown that the hydrolytic reaction, performed at 60 °C in acidic medium, leads to the regioselective cleavage of the amide bond involving the carboxylic group of histidine.

Diethanolamine Pd(II) complexes in bioorganic modeling as model systems of metallopeptidases and soybean lipoxygenase inhibitors.

The reaction of PdCl(2) with diethanolammonium chloride (DEAxHCl), in the molar ratio 1:2, affords the [HDEA](2)[PdCl(4)] complex (1). The hydrolytic activity of the novel Pd(II) complex 1 was tested in reaction with N-acetylated L-histidylglycine dipeptide (AcHis-Gly). Complex 1, as well as earlier prepared trans-[PdCl(2)(DEA)(2)] complex (2), and DEA, as their precursor, were tested for their in vitro free radical scavenging activity.