Temat: peptidomimetics - Prolib Integro

Skocz do pozycji: 1.

Tytuł:: Conformational analysis of amide derivatives of selected lactams and natural amino acids – the potential peptidomimetic building blocks
Analiza konformacyjna amidowych pochodnych wybranych laktamów i aminokwasów naturalnych : potencjalnych bloków budulcowych peptydomimetyków
Autorzy:: Owińska, Maria
Współwytwórcy:: Rys, Barbara
Dostawca treści:: Repozytorium Uniwersytetu Jagiellońskiego

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Skocz do pozycji: 2.

Tytuł:: Blood–Brain Barrier Penetration of Novel 4-Trifluoromethyl-Coumarin Hybrids with Antibacterial Properties as Potential Brain Therapeutics in the Context of Spatially Diverse Healthcare Systems
Autorzy:: Młotkowska, Patrycja
Kurylczyk, Apoloniusz
Głowacz, Krzysztof
Ostaszewski, Ryszard
Szlis, Michał
Marczyk, Michał
Kocot, Malwina
Krajewska-Pędzik, Anna
Misztal, Tomasz
Kowalczyk, Paweł
Gołębiewski, Marcin
Koszelewski, Dominik
Wypych, Aleksandra
Wydawca:: MDPI
Cytata wydawnicza:: Int. J. Mol. Sci. 2025, 26(19), 9655 // https://doi.org/10.3390/ijms26199655
Opis:: Kielanowski Institute of Animal Physiology and Nutrition Polish Academy of Sciences and the grant OPUS No. 2023/49/B/NZ7/02469 from Instite of Organic Chemistry Polish Academy of Sciences; Minister of Science under the “Regional Excellence Initiative”
Effective treatment of central nervous system (CNS) infections remains a major challenge, as most therapeutic agents do not efficiently cross the blood–brain barrier (BBB) and the blood–cerebrospinal fluid barrier (BCSFB). Coumarin derivatives are of particular interest due to their broad pharmacological activity, favorable safety profile, and potential to penetrate biological barriers. Eight novel coumarin-based peptidomimetics functionalized with trifluoromethyl or methyl scaffolds were synthesized and evaluated as antimicrobial agents with the ability to cross the blood–brain barrier. Antimicrobial activity of the investigated compounds was tested against Staphylococcus aureus and multiple Escherichia coli strains (K12, R2, R3, R4) using minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays. Cytotoxicity was assessed in vitro in BALB/c-3T3 mouse fibroblasts and αT3-1 pituitary gonadotrope cells using the MTT assay. In vivo studies were performed in sheep to assess transfer of the compounds from blood to cerebrospinal fluid (CSF). All synthesized derivatives demonstrated antimicrobial activity and acceptable cytotoxicity, comparable to those of clinically used antibiotics. CF3-modified coumarin peptidomimetics show promise as antimicrobial agents with the potential to penetrate the BBB/BCSFB. These findings support further investigation of coumarin-based scaffolds as a platform for the development of novel therapeutics for CNS infections.
Dostawca treści:: Repozytorium Centrum Otwartej Nauki

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Skocz do pozycji: 3.

Tytuł:: Peptydy i peptydomimetyki jako inhibitory tyrozynazy
Peptides and peptidomimetics as inhibitors of tyrosinase
Autorzy:: Ledwoń, Patrycja
Jewgiński, Michał
Latajka, Rafał
Tematy:: tyrozynaza
peptydy
peptydomimetyki
inhibitory tyrozynazy
kosmeceutyki
tyrosinase
peptides
peptidomimetics
tyrosinase inhibitors
cosmeceuticals; Pokaż więcej
Wydawca:: Polskie Towarzystwo Chemiczne
Powiązania:: https://bibliotekanauki.pl/articles/27310044.pdf Link otwiera się w nowym oknie
Opis:: The publication reviews the results on the tyrosinase inhibition capacity of a short peptide and peptide conjugates with known low molecular weight inhibitors of this enzyme. Tyrosinase is a widespread copper-dependent enzyme capable of catalyzing two reaction pathways for oxidizing monophenols to o-diphenols and o-diphenols to o-quinones. Despite the wide distribution in nature, the peptide chain that builds the catalytic cavity is relatively highly conserved for all organisms. As the research results collected in the work show, the creation of short peptide conjugates with known tyrosinase inhibitors, such as kojic acid, significantly reduces the toxicity of the inhibitor and improves its stability.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 4.

Tytuł:: Mystery of the Passerini Reaction for the Synthesis of the Antimicrobial Peptidomimetics against Nosocomial Pathogenic Bacteria
Autorzy:: Brodzka, Anna
Ostaszewski, Ryszard
Kowalczyk, Paweł
Kramkowski, Karol
Wavhal, Deepak S.
Gulko, Cezary
Koszelewski, Dominik
Wydawca:: MDPI
Cytata wydawnicza:: Int. J. Mol. Sci. 2024, 25, 8330 ; https://doi.org/10.3390/ijms25158330
Opis:: Medical University of Białystok Grant of National Science Center Opus 22 Nr 2021/43/B/NZ7/01903; National Science Center, Poland project OPUS No. 2019/33/B/ST4/01118
The first example of applying salicylaldehyde derivatives, as well as coumarin with the formyl group at the C8 position in its structure, as carbonyl partners in a three-component Passerini reaction, is presented. As a result of research on the conditions of the Passerini reaction, the important role of the hydroxyl group in the salicylaldehyde used in the course of the multicomponent reaction was revealed. When an aldehyde with an unprotected hydroxyl group is used, only two-component α-hydroxy amide products are obtained. In contrast, the use of acylated aldehyde results in three-component α-acyloxy amide products with high efficiency. The developed protocol gives access to structurally diversified peptidomimetics with good yield. The compounds were also evaluated as antimicrobial agents against selected strains of nosocomial pathogenic bacteria. The structure–activity relationship revealed that inhibitory activity is strongly related to the presence of the trifluoromethyl group (CF3) or the methyl group at the C4 position in an unsaturated lactone ring of the coumarin scaffold. MIC and MBC studies were carried out on eight selected pathogenic bacteria strains (Gram-positive pathogenic Staphylococcus aureus strain (ATCC 23235), as well as on Gram-negative E. coli (K12 (ATCC 25404), R2 (ATCC 39544), R3 (ATCC 11775), and R4 (ATCC 39543)), Acinetobacter baumannii (ATCC 17978), Pseudomonas aeruginosa (ATCC 15442), and Enterobacter cloacae (ATCC 49141) have shown that the tested compounds show a strong bactericidal effect at low concentrations. Among all agents investigated, five exhibit higher antimicrobial activity than those observed for commonly used antibiotics. It should be noted that all the compounds tested showed very high activity against S. aureus, which is the main source of nosocomial infections that cause numerous fatalities. Additionally, the cytotoxicity of sixteen derivatives was measured with the use of the MTT test on BALB/c3T3 mouse fibroblast cell lines. The cytotoxicity studies revealed that the tested substances exert a similar or lower effect on cell proliferation than that observed for commonly used antibiotics within the range of therapeutic doses. A parallel MTT assay using ciprofloxacin, bleomycin, and cloxacillin showed that these antibiotics are more cytotoxic when tested in mammalian cells, and cell viability is in the range of 85.0–89.9%. Furthermore, we have shown that the studied coumarin-based peptidomimetics, depending on their structural characteristics, are nonselective and act efficiently against various Gram-positive and Gram-negative pathogens, which is of great importance for hospitalised patients.
Dostawca treści:: Repozytorium Centrum Otwartej Nauki

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Skocz do pozycji: 5.

Tytuł:: Peptydomimetyki i foldamery aromatyczne w chemii biologicznej
Peptidomimetics and aromatic foldamers in biological chemistry
Autorzy:: Ledwoń, Patrycja
Staśkiewicz, Agnieszka
Jewgiński, Michał
Latajka, Rafał
Tematy:: inhibitors of enzymes
peptidomimetics
conformation
cosmeceutics
aromatic foldamers
SAR
inhibitor enzymu
peptydomimetyki
konformacja
kosmeceutyki
foldamery aromatyczne; Pokaż więcej
Wydawca:: Polskie Towarzystwo Chemiczne
Powiązania:: https://bibliotekanauki.pl/articles/2200585.pdf Link otwiera się w nowym oknie
Opis:: The interests of the research group working under the supervision of professor Rafał Latajka at the Department of Bioorganic Chemistry at the Wrocław University of Science and Technology are focused on several projects in the field of biological chemistry. Regardless of whether a given project concerns – the synthesis and activity of new enzyme inhibitors, peptides, peptidomimetics, or aromatic foldamers – the thread of correlation between the structure and activity of the studied systems always plays a pivotal role. In this article we are presenting current projects in our research group.
Dostawca treści:: Biblioteka Nauki

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Skocz do pozycji: 6.

Tytuł:: Fluorowany motyw w aktywnych biologicznie peptydomimetykach
Fluorinated motif in biologically active peptidomimetics
Autorzy:: Koroniak-Szejn, Katarzyna
Rapp, Magdalena
Tematy:: peptydomimetyki
fluoromimetyki
grupa trifluorometylowa
fluor
grupa fluorowinylowa
aktywność biologiczna
peptidomimetics
fluoromimetics
trifluorometyl group
fluorine
fluorovinyl group
biological activity; Pokaż więcej
Wydawca:: Polskie Towarzystwo Chemiczne
Powiązania:: https://bibliotekanauki.pl/articles/972282.pdf Link otwiera się w nowym oknie
Opis:: Incorporation of fluorine atom or fluoroalkyl group into molecules, often induces a remarkable effect upon the physical and chemical properties leading to significant changes of its reactivity [1-5], therefore this modification is often used in the synthesis of drugs and biologically active compounds [6, 7]. The change in reactivity has far-reaching consequences, affects bond energy in the molecule, acidity and alkalinity, hydrogen bond formation and the geometry of the molecule [1-5]. The change in acid-base properties and polarity forced by a fluorine or fluorinated motif in the modified amino acid or peptide molecule has already found numerous applications in bioisosteric mimetics [9]. In addition, using a fluorine atom as a probe, conformation determination and stereochemistry of receptor interaction become more effective due to the possibility of using ¹⁹F NMR spectroscopy. The stereoselective introduction of fluorine atoms can therefore be exploited as a conformational tool for the synthesis of shape-controlled functional molecules. Particular attention has been paid to fluorinated peptidomimetics due to the huge variety of their biological activity. Proteins play a significant role in drug design and synthesis. Peptide binding in living organisms is quite labile which is associated with the presence of proteolytic enzymes. Therefore, to prevent protein hydrolysis, new, modified compounds are thought to mimic the properties and functions of peptide bond. These types of compounds are called peptidomimetics. In this monograph, we will focus on the biologically active fluorinated peptidomimetics, in which the amide bond has been replaced by a fluorinated group and thus they can "mimic" peptide bond functions (pseudopeptides). Other peptidomimetics with typical amide bond, but in which the remaining part of the molecule has been modified by introducing a fluorinated group or fluorine (peptide analogs) will also be discussed. The main goal of this work, however, is to demonstrate the beneficial effect of fluorine on the properties of the modified compounds and associated with it consequences. The superior goal of this work, however, is to demonstrate the unique effect of fluorine on the properties of the target compounds and in the design of higher order structures reflecting a more sophisticated molecular construction that broadens biological mimesis.
Dostawca treści:: Biblioteka Nauki

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