Design, Synthesis and Biological Evaluation of Novel Promising Analgesics.

Introduction: An analysis of the literature on the painkillers long used in traditional medicine, which are isolated from plant materials, has shown that many of them are alkylamides of various carboxylic acids. This fact served as the basis for the study of a large group of N-alkyl-4- methyl-2,2-dioxo-1H-2λ,1-benzothiazine-3-carboxamides as potential new analgesics. The objects of the study were synthesized in the traditional way involving the initial conversion of 4-methyl- 2,2-dioxo-1H-2λ,1- benzothiazine-3-carboxylic acid to imidazolide, in which imidazolide was used as an acylating agent.

Resveratrol Effects on the Reproductive System in Ovariectomized Rats: Deciphering Possible Mechanisms.

Phytoestrogen resveratrol (R) has been demonstrated to benefit human reproductive health. However, R bioavailability and pharmacokinetics are still problematic under oral supplementation. We used an experimental vaginal gel with R and hyaluronic acid (HA) to improve bioavailability and pharmacokinetic properties.

Natural Dietary Compounds in the Treatment of Arsenic Toxicity.

Chronic exposure to arsenic (As) compounds leads to its accumulation in the body, with skin lesions and cancer being the most typical outcomes. Treating As-induced diseases continues to be challenging as there is no specific, safe, and efficacious therapeutic management. Therapeutic and preventive measures available to combat As toxicity refer to chelation therapy, antioxidant therapy, and the intake of natural dietary compounds.

Arctostaphylos uva-ursi L. leaves extract and its modified cysteine preparation for the management of insulin resistance: chemical analysis and bioactivity.

Bearberry (Arctostaphylos uva-ursi L.) is a perennial plant of the heather family (Ericaceae). The leaves are dominated by arbutin, phenol carbonic acids flavonoids, saponins, etc.

Quality by Design in optimizing the extraction of (poly)phenolic compounds from Vaccinium myrtillus berries.

Quality by Design was adopted for developing an effective extraction procedure of (poly)phenolic compounds from bilberry (Vaccinium myrtillus L.) fruits, using a pooled sample of berries from different regions of Ukraine. Mechanical solvent extraction, microwave-assisted extraction (MAE) and ultrasonic-assisted extraction (UAE) were investigated by screening matrices.

Effective Isolation of Picrocrocin and Crocins from Saffron: From HPTLC to Working Standard Obtaining.

Saffron is widely cultivated and used as a spice. Recently published data on the chemical composition and pharmacological potential of saffron determine its use in pharmacy and medicine. The proposed high-performance thin-layer chromatography (HPTLC) method allows good separation of 11 analytes.

Joint Task Force Core Competency Framework Adoption Process at a National Level: A Survey of Ukrainian-Based Clinical Research Professionals.

Background: The need to define core competencies for clinical research professionals has been widely recognized. And after the Joint Task Force have proposed Core Competency Framework in 2014 (Sonstein et al. in JAMA 28(3):17-23, 2014), it has been tested and implemented by a variety of researchers and practitioners worldwide, while Ukraine avoided implementing this until recently.

Computational studies on potential new anti-Covid-19 agents with a multi-target mode of action.

A compound that could inhibit multiple targets associated with SARS-CoV-2 infection would prove to be a drug of choice against the virus. Human receptor-ACE2, receptor binding domain (RBD) of SARS-CoV-2 S-protein, Papain-like protein of SARS-CoV-2 (PLpro), reverse transcriptase of SARS-CoV-2 (RdRp) were chosen for in silico study. A set of previously synthesized compounds (-) were docked into the active sites of the targets.

The Phytochemical Profile and Anticancer Activity of and Used in Estonian Ethnomedicine.

The aerial parts of L. and L. and the roots of have been used as traditional anticancer remedies in Estonian ethnomedicine.

Innovative GACP Approaches for Obtaining the Quality Iris hybrida Leaves for the Pharmaceutical Industry.

The ever-growing demand for active compounds of plant origin contributes to the implementation of cultivation methods for medicinal plants, according to the WHO guideline "Good Agricultural and Collection Practice (GACP) for Starting Materials of Herbal Origin" to obtain high-quality raw material with the stable phytocomponent composition. Therefore, the development of the cultivation and processing stages of Iris varieties leaves is necessary and promising. The present article showed the potential of proper cultivation with GACP recommendations on affecting the phenolic compounds content in Iris×hybrida hort.

Bioactive constituents of Iris hybrida (Iridaceae): Processing effect.

Iris genus plants are a valuable source of bioactive compounds, which are an important component for pharmaceutical development. The present article shows the potential for mineral nutrition with application of magnesium sulfate, iron chelates and potassium oxide affecting the phenolic compound contents in Iris hybrida 'Tsikavynka', I. hybrida 'Tambo' and I.

The Role of Pharmaceutical Scientists in the Formation of a Healthy Lifestyle as a Value Orientation.

This article focuses on the role pharmaceutical scientists play in achieving social well-being, in particular in the formation of a healthy lifestyle as a value orientation among students and the public in historical retrospect. The following set of research methods was used: a general scientific method, and a historical (chronological, logico-historical, retrospective), personalized, empirical method (including the questioning of pharmaceutical interns and the analytical processing of questionnaires). The territorial boundaries of the study cover Slobozhanshchyna, a historical and geographical region centered in Kharkiv.

1-Allyl-4-hydroxy-2,2-dioxo-N-(4-methoxyphenyl)-1H-2λ,1-benzothiazine-3-carboxamide: polymorphic transition due to grinding with the loss of the biological activity.

A study of two polymorphic forms of 1-allyl-4-hydroxy-2,2-dioxo-N-(4-methoxyphenyl)-1-2λ,1-benzothiazine-3-carboxamide (a structural analogue of piroxicam) has revealed some regularities in the crystal structure formation due to different evaporation rates from the tested solvents. The monoclinic polymorph crystallized from ethyl acetate is formed due to a large number of very weak C-H..

PROGNOSTIC SIGNIFICANCE OF METABOLISM INDICATORS OF CONNECTIVE TISSUE IN PATIENTS WITH UPPER URINARY TRACT OBSTRUCTION.

Objective: The aim: The aim of the study was a comparative analysis of indicators characterizing the state of connective tissue in patients with hydronephrosis due to upper urinary tract obstruction, with the presence and absence of recurrence after surgery.

Patients And Methods: Materials and methods: Levels of free and bound hydroxyproline, as well as the key mediator of fibrogenesis transforming growth factor-β1 in serum of patients with congenital and acquired obstructions were determined. Ratio peptide-bound and free hydroxyproline were calculated.

Comparative analysis of apocarotenoids and phenolic constituents of Crocus sativus stigmas from 11 countries: Ecological impact.

The chemical compositions of 15 saffron samples from 11 countries (Morocco, India, Italy, Spain, Germany, Switzerland, Iran, Lithuania, Ukraine, Australia, and Azerbaijan) were evaluated. The samples were analyzed regarding the impact of environmental factors on the composition of apocarotenoids and phenolic constituents. Quantification of saffron metabolites was carried out using high-performance liquid chromatography.

Analgesic properties of the dry combined extract BNO 1016 in leukotriene depended hyperalgesia.

Combined dry extract BNO 1016 is a herbal drug commonly used for rhinosinusitis therapy. It is known that a significant role in rhinosinusitis pathogenesis is played by an inflammatory reaction in maxillary sinuses of the nasal cavity. At the initial stage of any inflammation the largest impact is caused by leukotrienes.

Pharmacological Potential and Chemical Composition of Leaf Extracts.

L. (saffron) has been traditionally used as a food coloring or flavoring agent, but recent research has shown its potent pharmacological activity to tackle several health-related conditions. sp.

Application of closed kinematic chain exercises with eccentric and strength exercises for the shoulder injuries prevention in student rock climbers: a randomized controlled trial.

Purpose: The aim of this work to determine the influence of a program containing exercises in a closed kinematic chain, eccentric and strength exercises on injuries of students - rock climbers.

Methods: Participants in this study were 84 male amateur climbing students, aged 18-19, 40 athletes were in the intervention group and 44 in the control group. In the intervention group, the program for the injuries prevention has been stalled.

Impact of Compression Force on Mechanical, Textural, Release and Chewing Perception Properties of Compressible Medicated Chewing Gums.

Medicated chewing gums (MCGs) represent a beneficial platform for realizing drugs intended for dental prophylaxis and treatment. The present study aimed to investigate the impact of compression force on the mechanical, textural, release, and chewing perception characteristics of compressible MCGs with the combination of lysozyme hydrochloride (LH) and ascorbic acid (AsA). Four batches of MCGs were obtained on a laboratory single-punch tablet machine applying different forces, i.

Home pharmacological therapy in early COVID-19 to prevent hospitalization and reduce mortality: Time for a suitable proposal.

The COVID-19 pandemic is a highly dramatic concern for mankind. In Italy, the pandemic exerted its major impact throughout the period of February to June 2020. To date, the awkward amount of more than 134,000 deaths has been reported.

New luminometric method for quantification of biological sulfur nucleophiles with the participation of 9-cyano-10-methylacridinium salt.

Biologically active compounds containing sulfhydryl groups (RSHs: N-acetyl-l-cysteine, d-penicillamine, glutathione and acetylthiocholine chloride) were used to develop a luminometric method for their quantification. The title substrate capable of chemiluminescence (CL) was isolated in a highly pure state as a chloride salt (99.9% using RP-HPLC) and identified using mass spectrometry (ESI Q-TOF) and H NMR spectroscopy.

Investigation of the Rheological Properties of Ointment Bases as a Justification of the Ointment Composition for Herpes Treatment.

Objectives: Combinatorial drugs are among the leading pharmacotherapeutic agents, including those used for the treatment of herpetic infections, which require complex treatment. We have developed a soft dosage form of ointment, which includes acyclovir and miramistin, which have antimicrobial, anti-inflammatory, and local immunoadjuvant activity. The study aimed to investigate the rheological properties of ointment bases in order to substantiate the composition of a soft dosage form with antiviral effect using the active ingredients miramistin and acyclovir.

Realities of Pharmaceutical Compounding in the Republic of Uzbekistan.

The development of compounding science in the Republic of Uzbekistan began in ancient times. The emergence of medical science on the territory of modern Uzbekistan was associated with the activities of the famous physician Ibn Sina (Avicenna). His Canon of Medicine is still considered the main source of medical knowledge in the world.