Three Ecological Models to Evaluate the Effectiveness of spp. for Suppressing Aflatoxigenic and .

Chemical pesticides help reduce crop loss during production and storage. However, the carbon footprints and ecological costs associated with this strategy are unsustainable. Here, we used three in vitro models to characterize how different species interact with two aflatoxin producers, and , to help develop a climate-resilient biological control strategy against aflatoxigenic species.

2-Oxabicyclo[2.1.1]hexanes: Synthesis, Properties, and Validation as Bioisosteres of ortho- and meta-Benzenes.

We have developed a general and practical approach towards 2-oxabicyclo[2.1.1]hexanes with two and three exit vectors via an iodocyclization reaction.

2-Oxabicyclo[2.1.1]hexanes as saturated bioisosteres of the ortho-substituted phenyl ring.

The ortho-substituted phenyl ring is a basic structural element in chemistry. It is found in more than three hundred drugs and agrochemicals. During the past decade, scientists have tried to replace the phenyl ring in bioactive compounds with saturated bioisosteres to obtain novel patentable structures.

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.

Actions speak louder than words. Dilogy on the decision of the journal Acta Biochimica Polonica to exclude Russian science from publishing.

For the time being, as one of only a few journals world-wide, the scientific journal Acta Biochimica Polonica (henceforth ABP) has decided not to accept manuscripts submitted by authors affiliated with Russian institutions. This is a strong symbolic act of solidarity with Ukraine being assaulted by Russia. The questions are, however, how this unprecedented boycott of researchers from publishing because their nation leads a criminal war could be justified, and how this harsh action is in accordance with fundamental principles of science and its system.

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..

Saturated Bioisosteres of ortho-Substituted Benzenes.

Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated.

Biological properties of two enantiomorphic forms of N-(2,6-dimethylphenyl)-4-hydroxy-2,2-dioxo-1H-2λ,1-benzothiazine-3-carboxamide, a structural analogue of piroxicam.

The title benzothiazine-3-carboxamide, CHNOS, crystallized in two enantiomorphic crystal forms with the space groups P3 and P3 despite the absence of a classic stereogenic atom. The molecular structures are mirror images of each other. Only one sulfonyl O atom takes part in intramolecular hydrogen bonding as a proton acceptor and this atom is different in the two enantiomorphic structures.

[NON-CARDIAL EFFECTS OF SGLT2 INHIBITORS (REVIEW)].

The article reveals the efficacy and safety aspects of a new class of antidiabetic drugs - SGLT2 inhibitors. The results of clinical and experimental studies of the principle of renal glucose reabsorption inhibition usage in the treatment of type 2 diabetes are presented in the article. Drugs of this class offer a new, non-insulin-dependent mechanism of action, lack of negative effect on body weight, favorable pharmacokinetic properties and good tolerance.

EXPERIMENTAL STUDY OF PAIN-RELIEVING MECHANISMS OF 4-[4-OXO-(4H)-QUINAZOLIN-3-YL]-BENZOIC ACID (PK-66 COMPOUND).

An in-depth study of the pharmacological properties of 4-[4-oxo-(4h)-quinazolin-3-yl]-benzoic acid as an analgesic agent established that it had a sufficiently high analgesic effect on models of somatic and neuropathic pain syndromes. Study objective was to study the mechanisms of analgesic action of PK-66 compound in rats using the pharmacological analysis. We evaluated the mechanisms of analgesic effect of PK-66 (1 mg/kg, intraperitoneal) compound on the thermal irritation model on Hours 1, 2, 4 and 6 after administration of study compounds.

INFLUENCE OF H2S DONOR ON CHANGES IN THE CELL CYCLE AND THE APOPTOSIS PROCESS INDUCED BY DICLOFENAC IN THE RAT GASTRIC MUCOSA.

The purpose of this work was to study the effect of concomitant administration of sodium hydrosulfide and diclofenac sodium on the parameters cell cycle of the gastric mucosa cells by DNA flow cytometry. The experiments were performed on 24 white rats of Wistar straints. The parameters of the cell cycle of cells of the gastric mucosa of rats were determined by the method of flow-through DNA-cytometry.

THE STATE OF THE CYSTATHIONINE GAMMA-LYASE / H2S SYSTEM IN THE LIVER AND SKELETAL MUSCLES OF RATS WITH HYPERCHOLESTEROLEMIA UNDER SIMVASTATIN ADMINISTRATION.

In studies on 94 male Wistar rats changes in the hydrogen sulfide content (H2S) and cystathionine γ-lyase (CSE) in the liver and skeletal muscles in hypercholesterolemia under simvastatin treatment were assessed, as well as the effect of propargylglycine (PAG) on hepato- and myotoxicity of simvastatin. It was determined, that simvastatin inhibited the CSE-mediated synthesis of H2S in the main target organs. This negatively affected their biochemical and functional status.

Synthesis, Crystal Structure, and Biological Activity of Ethyl 4-Methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate Polymorphic Forms.

Continuing the search for new potential analgesics among the derivatives of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid, the possibility of obtaining its esters by the alkylation of the corresponding sodium salt with iodoethane in dimethyl sulfoxide (DMSO) at room temperature was studied. It was found that under such conditions, together with the oxygen atom of the carboxyl group, a heteroatom of nitrogen is also alkylated. Therefore, the product of the reaction studied is a mixture of ethyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate (major) and its 1-ethyl-substituted analog (minor).

4-Methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxylic Acid. Peculiarities of Preparation, Structure, and Biological Properties.

In order to determine the regularities of the structure-analgesic activity relationship, the peculiarities of obtaining, the spatial structure, and biological properties of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid and some of its derivatives have been studied. Using nuclear magnetic resonance (NMR) spectroscopy and X-ray diffraction analysis, it has been proven that varying the reaction conditions using alkaline hydrolysis of methyl 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylate makes it possible to successfully synthesize a monohydrate of the target acid, its sodium salt, or 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine. The derivatographic study of the thermal stability of 4-methyl-2,2-dioxo-1-2λ⁶,1-benzothiazine-3-carboxylic acid monohydrate has been carried out; based on this study, the optimal conditions completely eliminating the possibility of unwanted decomposition have been proposed for obtaining its anhydrous form.

Peptide oligomers from ultra-short peptides using sortase.

Sortase A catalyzed ligation of ultra-short peptides leads to inter/intra-molecular transpeptidation to form either linear or cyclic oligomers dependent upon the peptide length. Cyclic peptides were the main products for peptides with more than 15aa. However, for ultra-short (<15aa) peptides, cyclic oligomers became predominant in prolonged reactions.

[The Influence of Regulative Factors on Mycobiota Structure of Quercus robur L. Acorns During Storage].

Aim: To study mycobiota structure of Quercus robur acorns during storage and its ozone and wax treatment infuence on fungi.

Methods: Mycological, physical and mathematical methods were used to investigation.

Results: The lowest similarity of mycobiota species structure was observed between acorns treated with ozone and ones overwintered under nature conditions (S=0.

Sortase A Mediated Protein Modifications and Peptide Conjugations.

Bioactive peptides regulate many physiological processes, acting at some sites as endocrine or paracrine signals and at others as neurotransmitters or growth factors, and show useful properties for human health, including antimicrobial, antifungal, antiviral, and antitumor activities. Although most peptides can be produced using the molecular biology approach, they are produced in limited quantities at high costs and associated with some difficulties in purification and isolation. In addition, some peptides with special structures, such as cyclic peptides, can hardly be produced by the biological method.

[Peculiarities of mortmass mycobiota formation in soft-deciduous young forests on old-tillage soils of the Chernihiv Polissya].

Thirty eight species of fungi were identified as a result of mycological analysis of 180 mortmass samples of Betulapendula Routh. and Populus tremula L. Mortmass mycobiota of B.

[Formation peculiarities of Quercus robur L. acorn mycobiota under conditions of Kyiv Polissya].

The structure of mycobiota (epiphytic and from inner tissues) of Q. robur acorns (580 samples) under conditions of Kyiv Polissya was studied. Acorn samples were collected from oak trees during vegetation period.

Lytic peptides with improved stability and selectivity designed for cancer treatment.

Lytic peptides are a group of membrane-acting peptides, which have excellent activity to drug-resistant cells. In this study, the stability and tumor selectivity of newly designed pH-activated lytic peptides were studied. We found that despite varied secondary structures, pH-induced structure changes could not be directly linked to the activity and pH sensitivity of peptides.

Mutagenesis of tGCN5 core region reveals two critical surface residues F90 and R140.

Tetrahymena General Control Non-Derepressor 5 (tGCN5) is a critical regulator of gene transcription via acetylation of histones. Since the acetylation ability has been attributed to the "core region", we perform mutagenesis of residues within the tGCN5 "core region" in order to identify those critical for function and stability. Residues that do not participate in catalysis are identified, mutated and characterized for activity, structure and thermodynamic stability.

Incorporation of unnatural amino acids for synthetic biology.

The challenge of synthetic biology lies in the construction of artificial cellular systems. This requires the development of modular "parts" that can be integrated into living systems to elicit an artificial, yet programmed, response or function. The development of methods to engineer proteins bearing unnatural amino acids (UAAs) provides essential components that may address this challenge.

Positional effects of monofluorinated phenylalanines on histone acetyltransferase stability and activity.

To explore the impact of global incorporation of fluorinated aromatic amino acids on protein function, we investigated the effects of three monofluorinated phenylalanine analogs para-fluorophenylalanine (pFF), meta-fluorophenylalanine (mFF), and ortho-fluorophenylalanine (oFF) on the stability and enzymatic activity of the histone acetyltransferase (HAT), tGCN5. We selected this set of fluorinated amino acids because they bear the same size and overall polarity but alter in side chain shape and dipole direction. Our experiments showed that among three fluorinated amino acids, the global incorporation of pFF affords the smallest perturbation to the structure and function of tGCN5.