Bioisosteric Replacement in the Search for Biologically Active Compounds: Design, Synthesis and Anti-Inflammatory Activity of Novel [1,2,4]triazino[2,3-c]quinazolines.

Designing novel biologically active compounds with anti-inflammatory properties based on condensed quinazolines is a significant area of interest in modern medicinal chemistry. In the present study, we describe the development of promising new bioactive molecules through the bioisosteric replacement of a carbon atom with a sulfur atom in anti-inflammatory agents, specifically 3-methyl-2-oxo-2-[1,2,4]triazino[2,3-]quinazolin-6-yl)butanoate. Design and synthetic studies have led to the series of previously unknown substituted 2-[((3-R-2-oxo-2-[1,2,4]triazino[2,3-]quinazolin-6-yl)methyl)thio]carboxylic acids and their esters.

Effects of Pirimiphos-Methyl on Non-Target Invertebrates.

The effects of pirimiphos-methyl have previously been assessed on blood-sucking insect species, pollinating insects, and target crop pest species. The sensitivity of non-target zoophagous and saprophage species to this insecticide remains largely unstudied. In laboratory conditions, we assessed the susceptibility of 43 species of invertebrates to pirimiphos-methyl.

O,S,Se-containing Biginelli products based on cyclic β-ketosulfone and their postfunctionalization.

A one-pot three-component Biginelli synthesis of dihydropyrimidinones/thiones/selenones via acetic acid or solvent-free Yb(OTf)-catalyzed tandem reaction of β-ketosulfone (dihydro-2-thiopyran-3(4)-one-1,1-dioxide), an appropriate urea, and arylaldehyde has been developed. The reaction proceeds with high chemo- and regioselectivity to give diverse DHPMs in reasonable yields up to 95%. Moreover, an SO-containing analogue of anticancer drug-candidate enastron (SO vs C=O) was obtained by using the here reported method in gram scale.

Effects of Organic Xenobiotics on Larvae and Their Parasite .

Environmental contamination with xenobiotics affects organisms and the symbiotic relations between them. A convenient object to study relationships between parasites and their hosts is the host-parasite system " Linnaeus, 1758 (Coleoptera, Tenebrionidae) (Hammerschmidt, 1838) Stein, 1848 (Eugregarinorida, Gregarinidae)". For this experiment, we took 390 larvae and 24 organic compounds.

Repellent and Attractant Activities of Organic Compounds on Female and Male (Coleoptera, Staphylinidae).

The use of organic compounds in different spheres of human activity is accompanied by their influx to and accumulation in the environment. The negative impact of those compounds can be one of the reasons for a decline in populations and biodiversity of aboveground invertebrates. Chemical compounds can potentially cause a variety of effects (attractant or repellent) on insects, including species of the Staphylinidae family.

Immunophysiological State of Dogs According to the Immunoregulatory Index of Their Blood and Spleens.

In this study, the immunological characteristics of a dog's body were established, allowing for a quick reaction to any changes in the immune status and the development of an immunodeficiency state. The immunoregulatory blood index was determined to indicate the ratio of T-helpers and T-suppressors. The immunoregulatory index of the spleen was determined as the ratio of CD4+ cells to CD8+ cells in the field of view of a microscope (eyepiece 10, objective 40) after obtaining histological preparations according to generally accepted methods.

A non-extraction sequential injection method for determination of loratadine using formation of its ion-association complex with bromocresol purple in acetonitrile.

The formation of an ion-association complex (IA) between sulfonephthalein dye and basic nitrogen-containing compound in an organic solvent medium has been for the first time used to develop an automated SIA method. In highly polar aprotic solvents, the tautomeric equilibrium for such dyes is strongly shifted towards the colorless lactonic form. The addition of a basic nitrogen-containing substance leads to the formation of IA with a highly colored quinonoid form, which is accompanied by an increase in the absorbance of the dye band at approximately 400 nm.

5+1-Heterocyclization as preparative approach for carboxy-containing triazolo[1,5-c]quinazolines with anti-inflammatory activity.

Present article is devoted to the purposeful search of novel anti-inflammatory agents among carboxyl-containing partially hydrogenated [1,2,4]triazolo[1,5-с]quinazolines and products of their tandem cyclization. It has been shown that target compound's could be obtained via interaction between [2-(3-R-1H-1,2,4-triazol-5-yl)phenyl]amines and oxo-containing carboxylic acids and their esters of various structure. The structures of synthesized compounds were verified by appropriate methods, the features of NMR-spectra patterns were discussed as well.

Survival of Nematode Larvae after Treatment with Eugenol, Isoeugenol, Thymol, and Carvacrol.

Background: Helminthiases inflict annual losses on the meat and dairy livestock industries. The commonest species of ruminant parasites are the nematodes: and , which lay eggs in the intestine and enter the feces. There, the eggs develop into larvae, which when voided with the feces crawl onto plants.

Influence of Inula helenium rhizomes and Matricaria chamomilla inflorescences on the biochemical and physiological parameters in male rats fed a high-fat diet.

Background: Pharmacological correction of a high-fat diet is of great interest to prevent the development of obesity and hypertension. More and more research is being done on the preventive use of medicinal herbs for excess caloric intake.

Objective: The aim of this study was to determine the general physiological effect of I.

Direct immersion single-drop microextraction combined with fluorescence detection using an optical probe. Application for highly sensitive determination of rhodamine 6G.

The use of an optical probe for fluorescence detection combined with direct immersion single-drop microextraction has been demonstrated as an innovative approach. The optical probe served both as a drop holder for extractant and as a measuring device which made it possible to eliminate the use of cuvettes. A laser and a light emitting diode (LED) were tested as possible light sources.

1-Azaspiro[3.3]heptane as a Bioisostere of Piperidine.

1-Azaspiro[3.3]heptanes were synthesized, characterized, and validated biologically as bioisosteres of piperidine. The key synthesis step was thermal [2+2] cycloaddition between endocyclic alkenes and the Graf isocyanate, ClO S-NCO, to give spirocyclic β-lactams.

The Development of the Verb System in the Ontological Opposition of Space and time in the Indo-European Language Family.

The research investigates the system of the Indo-European verb through the lens of Gustave Guillaume's psycho-systematics theory. By employing "mental vision" and phenomenology, the linguistic concept was explored at multiple levels: the surface structure of language in speech and the deeper level within the Indo-European language system. The analysis of the tense system of the Indo-European verb starts with the ontologisation of a person in both the world and language.

Effect of Rhizome and Fruit Peel on the Metabolic Processes and Physiological Activity of Rats Fed with Excessively Fat Diet.

Research Background: (golden root) and (pomegranate), as well as a number of other species of medicinal plants, exert an array of biological effects: adaptogenic, antioxidant and anti-inflammatory. However, there are not enough contemporary studies of their influence on metabolic processes, especially in cases of imbalanced diet. Lipid dysregulation is the main reason for many diseases, including obesity, cardiovascular disorders, non-alcoholic fatty liver disease, hypertension, atherosclerosis and insulin resistance.

Consecutive spectrophotometric determination of phosphate and silicate in a sequential injection lab-at-valve flow system.

A new highly sensitive and selective sequential injection lab-at-valve spectrophotometric method for the consecutive determination of silicate and phosphate is described. The proposed method is based on the formation of specific ion-association complexes (IAs) of 12-heteropolymolybdates of phosphorus and silicon (12-MSC) with Astra Phloxine. The addition of an external reaction chamber (RC) to the SIA manifold made it possible to significantly improve the conditions for the formation of the analytical form used.

LC-MS/MS bioanalytical method for the quantitative analysis of nifedipine, bisoprolol, and captopril in human plasma: Application to pharmacokinetic studies.

In this study, the development and validation of an accurate and highly sensitive LC-MS/MS method were performed for the estimation of nifedipine, bisoprolol and captopril in real human plasma. Liquid-liquid extraction using tert-butyl methyl ether was efficiently applied for extraction of the analytes from plasma samples. The chromatographic separation was carried out using an isocratic elution mode on the X-terra MS C column (4.

Impact of Vitamin D3 on Carbonyl-Oxidative Stress and Matrix Metalloproteinases after Acute Intracerebral Hemorrhage in Rats with Type 2 Diabetes Mellitus.

Introduction: Diabetes mellitus is associated with the development of carbonyl-oxidative stress (COS) and an increased risk of a cerebral hemorrhage. Vitamin D3 is considered an additional drug to have an impact on COS and proteolysis in the extracellular matrix.

Objective: The study aimed to evaluate the impact of D3 on the COS-markers and matrix metalloproteinases MMP2/MMP9 activity after acute intracerebral hemorrhage (ICH) in rats with experimental type 2 diabetes mellitus (Т2DM) compared to metformin (Met).

Innovated single flush on-line solid-phase extraction in bead injection format for flow programming-based determination of creatinine in human urine.

Reaction-based assays are commonly automated and miniaturized via flow analysis. However, aggressive reagents can affect or destroy even the chemically resistant manifold during long-term use. Using on-line solid-phase extraction (SPE) can eliminate this drawback and allow for high reproducibility and further advanced automation, as presented in this work.

5,6-Dihydrotetrazolo[1,5-c]quinazolines: Toxicity prediction, synthesis, antimicrobial activity, molecular docking, and perspectives.

Antimicrobial resistance is a never-ending challenge, which should be considered seriously, especially when using unprescribed "over-the-counter" drugs. The synthesis and investigation of novel biologically active substances is among the directions to overcome this problem. Hence, 18 novel 5,6-dihydrotetrazolo[1,5-c]quinazolines were synthesized, their identity, purity, and structure were elucidated by elemental analysis, IR, LC-MS, Н, and C NMR spectra.

Tacrolimus and Azole Derivatives of Agricultural and Human Health Importance: Prediction of ADME Properties.

Introduction: Agricultural chemicals are impacting health nowadays. Recently, promising synergistic antifungal interaction between tacrolimus and some azole compounds was studied.

Objective: To determine ADME parameters, potential side effects of test substances to reduce time and resources in the future.

Features of Kidney Function in Patients With Comorbidity of Arterial Hypertension and Chronic Obstructive Pulmonary Disease.

Background and objective Chronic kidney disease (CKD) and hypertension are closely linked in terms of cause and effect. Decreased renal function is usually associated with increased blood pressure, and a steady increase in blood pressure accelerates the decline in renal function. In this study, we aimed to investigate laboratory parameters of renal function - blood creatinine level, urine creatinine level, urea blood level, urine albumin level, and in particular, serum cystatin C level - as early predictors of kidney damage and assess the filtration function of the kidneys based on the glomerular filtration rate (GFR) in patients with isolated arterial hypertension, those with a comorbid pathology of hypertension and chronic obstructive pulmonary disease (COPD).

Promising medicinal plants for treatment of helminths of bison.

Bison bonasus (Linnaeus, 1758) and B. bison (Linnaeus, 1758) are mammals placed in the Red Book of the International Union for Conservation of Nature. Populations of those species of animals are under threat of extinction.

Metallophenolomics: A Novel Integrated Approach to Study Complexation of Plant Phenolics with Metal/Metalloid Ions.

Plant adaptive strategies have been shaped during evolutionary development in the constant interaction with a plethora of environmental factors, including the presence of metals/metalloids in the environment. Among adaptive reactions against either the excess of trace elements or toxic doses of non-essential elements, their complexation with molecular endogenous ligands, including phenolics, has received increasing attention. Currently, the complexation of phenolics with metal(loid)s is a topic of intensive studies in different scientific fields.

A new approach for sulfite determination by headspace liquid-phase microextraction with an optical probe.

A new approach of headspace liquid-phase microextraction with an optical probe (HS-LPME-OP), which solves the problem of the extraction phase retention in the hole of the optical probe and provides the possibility of simpler, more precise and reliable online processing of the analytical signal, was used for sulfite determination. A 1 × 10 M 5,5'-dithiobis-(2-nitrobenzoic) acid (DTNB) solution was used as an acceptor phase. It was placed in a plastic vial fixed in the headspace above the analyte solution.