Background: The unique ability of piperidine to combine with various molecular fragments makes it possible to use its chemical structure to create new drugs with potential pharmacological effects. However, preliminary studies are required to predict the activity of new compounds in order to determine the direction of further preclinical studies. Aim: This study aims at determining the potential targets and spectrum of biological activity of new piperidine derivatives by the in silico method. Material and methods: Prediction of the effects on targets and the spectrum of biological activity of three new piperidine derivatives synthesized at the Bekturov Institute of Chemical Sciences JSC was analyzed in this study. The chemical structures of these compounds were studied in silico using the web tool SwissTargetPrediction to identify the most likely protein targets. PASS (Prediction of Activity Spectra for Substances) online tool was used to predict the possible pharmacological activity of the studied compounds. Results: New modified piperidine derivatives are able to affect different enzymes, receptors, transport systems, voltage-gated ion channels, thereby providing a wide range of biological activities applicable in various fields of medicine. These substances represent interest in the treatment of cancer, central nervous system diseases, as local anesthetic, antiarrhythmic and antimicrobial agents, and are promising for pharmacological activity demonstration in preclinical studies. Conclusion: A comprehensive analysis of the above results leads to the conclusion that the compounds under study should be considered as potential substances for the design of new highly effective medicinal agents with a wide range of practical applications.

The chemical structure of piperidine has a unique ability to combine with other molecular fragments. This fact makes it possible to actively use it as an effective basis for the creation of new drug-like substances. Thus, the aim of the current investigation was to study the acute toxicity, local anesthetic potency, and antiarrhythmic activity of the two new synthesized piperidine derivatives under laboratory codes LAS-286 and LAS-294 (local anesthetic substances). The Bulbring & Wajda animal model and method of determining the nociception threshold during electrical stimulation was used to investigate the action of the substance during infiltration anesthesia. An antiarrhythmic activity was observed by the aconitine-induced rat arrhythmia model. Additionally, these compounds were studied in relation to molecular docking to delineate the structure-activity relationships. The tested piperidine derivatives had a low toxicity in the subcutaneous and intravenous administration routes. The experimental results showed a higher prolonged and pronounced local anesthetic activity for LAS-286 at a 0.5% concentration, compared to the reference preparations. The low dosage of 0.1 mg/kg of LAS-294 demonstrated a pronounced preventive antiarrhythmic effect in 90% of cases on the development of mixed arrhythmia, caused by aconitine. The results of molecular docking confirmed a higher binding affinity of the tested piperidines with the Na_v1.4 and Na_v1.5 macromolecules. The results of the present study are very promising, because these piperidines have shown a high biological activity, which can suggest a potential therapeutic application in the future.

Current research on the synthesis of isonicotinic acid (INA) has focused on the development of catalysts by mixing transition metal oxides such as vanadium, titanium and zirconium in the desired molar ratio. These materials have good catalytic activity (CA) but have drawbacks, including low resistance to deactivation and limited ability to control reaction selectivity. In the present study, two- and three-component catalysts containing vanadium were successfully synthesized and their compositions and properties were studied. The experimental results showed that the efficiency of V-Ti-Mn-O catalyst was superior to V-Ti-O. Selectivity analysis showed that V-Ti-Mn-O was the most efficient catalyst, reaching a maximum value of 67.17% at 320 °C. Scanning electron microscope (SEM), Raman spectroscopy and X-ray diffraction (XRD) were used to characterize the catalysts. The corresponding experimental results showed that the superior performance of the V-Ti-Mn-O catalyst was attributed to both the smaller size of the catalyst particles and their more uniform distribution. In the oxidation of 4-methylpyridine (4-MP), the V-Ti-O catalyst showed lower CA and stability compared to the V-Ti-Mn-O catalyst, which can be attributed to its limited CA and potential deactivation at higher temperatures, probably due to excessive oxidation.

This paper presents the results of an investigation into the catalytic activity and selectivity of rhodium-based catalysts supported on natural zeolite clinoptilolite from the Shankanai field (Kazakhstan) in the dehydrogenation of light alkanes from associated petroleum gas (APG). Three modifications of the catalyst have been studied: basic 1%Rh/HCpt, modified with tin 1%Rh/10%SnO/HCpt, and combined with additives of tin and potassium 1%Rh/10%SnO/5%K₂O/HCpt. It has been shown that the addition of tin contributes to increased thermal stability and a decreased coking rate, while the addition of potassium suppresses side reactions (cracking and isomerization), increasing the selectivity for olefins. The highest yield of olefins (~30%) is achieved with the 1%Rh/10%SnO/5%K₂O/HCpt catalyst in the presence of water vapor. Using scanning electron microscopy (SEM) and high-resolution transmission electron microscopy (HRTEM), improved distribution of active components and reduced catalyst deactivation have been confirmed. The obtained data demonstrate the potential of the developed systems for the efficient processing of APG and the selective synthesis of olefins.

The study investigates the catalytic activity of vanadium-containing catalysts in the selective oxidation of 4-methylpyridine (4-MP) in the gas phase. V-Cr, V-Ti, and V-Ti-Cr catalysts were synthesised and studied. The phase composition and structural features of the catalysts were determined by X-ray diffraction (XRD) and Raman spectroscopy, and their thermal stability was investigated using thermogravimetric analysis (TGA/DTA). Textural characteristics were evaluated by low-temperature nitrogen adsorption–desorption (BET, BJH), surface morphology was studied using scanning electron microscopy (SEM), and the distribution of elements was investigated using energy-dispersive X-ray spectroscopy (EDX). The chemical composition of the catalysts was determined using inductively coupled plasma atomic emission spectrometry (ICP-OES) and catalytic activity was evaluated in the selective gas-phase oxidation reaction of 4-methylpyridine in the temperature range 280–380 °C. It was found that an increase in temperature is accompanied by an increase in the conversion of 4-methylpyridine, but at the same time, deep oxidation reactions intensify. The best result is achieved on the V-Ti-Cr catalyst, for which the conversion of 4-MP reaches 86.88% and the selectivity is 73.06% at 320 °C. However, V-Ti provides moderate stable performance, while V-Cr demonstrates relatively low efficiency. Thus, it can be concluded that the nature of the temperature dependence of 4-methylpyridine conversion reflects the different nature of the active centres and their stability.

Piperidine derivatives are of interest to researchers considering piperidines as an effective scaffold for the synthesis of new compounds. The aim of this research was to investigate the acute toxicity and local anesthetic activity of new synthesized 4-(Naphthalen-1-yloxy)but-2-yn-1-yl)-containing piperidine derivatives. Acute toxicity tests were performed on outbred laboratory mice by subcutaneous injection of increasing concentrations of the test solutions. An initial investigation of local anesthetic activity during infiltration anesthesia was performed on guinea pigs using the Bulbring & Wajda animal model. An in-depth study of the efficacy of the most active compound was performed on a model of infiltration anesthesia of the rabbit’s abdominal wall by determining the threshold of nociception during electrical stimulation. Studied new piperidine derivatives are low-toxic substances, which are confirmed by the results of an acute toxicity study. At the stage of the primary study of local anesthetic activity during infiltration anesthesia on the experimental Bulbring and Wajda model, the LAS-251 compound showed the greatest activity, surpassing the reference drugs in terms of anesthesia index, duration of full anesthesia and total duration of action. At the stage of in-depth study, despite a longer latency period, LAS-251 has a local anesthetic effect longer than procaine and is slightly inferior to lidocaine. Results of present study are promising because complex 1-(4-(naphthalen-1-yloxy)but-2-yn-1-yl)-4-phenylpiperidine (LAS-251) with cyclodextrin showed high local anesthetic activity. This new piperidine derivative is future-oriented for prospective studies of other types of anesthesia, as a potential medicinal substance for therapeutic use in the future.