Search Results - "Mucha, Artur"
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Synthesis and modifications of phosphinic dipeptide analogues
Published in Molecules (15-11-2012)“…Pseudopeptides containing the phosphinate moiety (-P(O)(OH)CH(2)-) have been studied extensively, mainly as transition state analogue inhibitors of…”
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Antibacterial Activity of Ebselen
Published in International journal of molecular sciences (13-01-2023)“…Ebselen is a low-molecular-weight organoselenium compound that has been broadly studied for its antioxidant, anti-inflammatory, and cytoprotective properties…”
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Recent developments in the synthesis and applications of phosphinic peptide analogs
Published in Bioorganic & medicinal chemistry letters (01-05-2019)“…[Display omitted] •Phosphinic peptides are transition state inhibitors of Zn-proteases and ligases.•Binding to the active sites involves metal complexation and…”
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P1' Residue-Oriented Virtual Screening for Potent and Selective Phosphinic (Dehydro) Dipeptide Inhibitors of Metallo-Aminopeptidases
Published in Biomolecules (Basel, Switzerland) (24-04-2020)“…Designing side chain substituents complementary to enzyme binding pockets is of great importance in the construction of potent and selective phosphinic…”
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Recent Developments in Peptidyl Diaryl Phoshonates as Inhibitors and Activity-Based Probes for Serine Proteases
Published in Pharmaceuticals (Basel, Switzerland) (10-06-2019)“…This review presents current achievements in peptidyl diaryl phosphonates as covalent, specific mechanism-based inhibitors of serine proteases. Along three…”
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N -Benzyl Residues as the P1' Substituents in Phosphorus-Containing Extended Transition State Analog Inhibitors of Metalloaminopeptidases
Published in Molecules (Basel, Switzerland) (22-09-2020)“…Peptidyl enzyme inhibitors containing an internal aminomethylphosphinic bond system (P(O)(OH)-CH -NH) can be termed extended transition state analogs by…”
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A tribute to Prof. Pawel Kafarski
Published in ARKIVOC (10-10-2011)Get full text
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Aminophosphinates against Helicobacter pylori ureolysis-Biochemical and whole-cell inhibition characteristics
Published in PloS one (09-08-2017)“…Urease is an important virulence factor from Helicobacter pylori that enables bacterial colonization of human gastric mucosa. Specific inhibition of urease…”
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Bis(aminomethyl)phosphinic Acid, a Highly Promising Scaffold for the Development of Bacterial Urease Inhibitors
Published in ACS medicinal chemistry letters (12-02-2015)“…Inhibitors of bacterial ureases are considered to be promising compounds in the treatment of infections caused by Helicobacter pylori in the gastric tract…”
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P-C bond formation in reactions of Morita-Baylis-Hillman adducts with phosphorus nucleophiles
Published in ARKIVOC (11-10-2016)Get full text
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Structural basis for the inhibition of the essential Plasmodium falciparum M1 neutral aminopeptidase
Published in Proceedings of the National Academy of Sciences - PNAS (24-02-2009)“…Plasmodium falciparum parasites are responsible for the major global disease malaria, which results in >2 million deaths each year. With the rise of…”
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Structure of the Plasmodium falciparum M17 aminopeptidase and significance for the design of drugs targeting the neutral exopeptidases
Published in Proceedings of the National Academy of Sciences - PNAS (09-02-2010)“…Current therapeutics and prophylactics for malaria are under severe challenge as a result of the rapid emergence of drug-resistant parasites. The human malaria…”
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Diethyl boronobenzylphosphonates as substrates in Petasis reaction
Published in ARKIVOC (16-08-2016)Get full text
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Identification of Phosphinate Dipeptide Analog Inhibitors Directed against the Plasmodium falciparum M17 Leucine Aminopeptidase as Lead Antimalarial Compounds
Published in Journal of medicinal chemistry (29-11-2007)“…Previous studies have pinpointed the M17 leucyl aminopeptidase of Plasmodium falciparum (PfLAP) as a target for the development of new antimalarials. This…”
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Addition of H-phosphonates to quinine-derived carbonyl compounds. An unexpected C9 phosphonate-phosphate rearrangement and tandem intramolecular piperidine elimination
Published in Beilstein journal of organic chemistry (17-04-2014)“…The Abramov reaction, a base-catalyzed nucleophilic addition of dialkyl H-phosphonates (phosphites) to carbonyl compounds, was performed with oxidized quinine…”
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Individual stereoisomers of phosphinic dipeptide inhibitor of leucine aminopeptidase
Published in Bioorganic & medicinal chemistry (01-03-2008)“…First successful separation of all four stereoisomers of a phosphinic acid pseudodipeptide allowed to determine the inhibitory activity of the…”
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The M18 Aspartyl Aminopeptidase of the Human Malaria Parasite Plasmodium falciparum
Published in The Journal of biological chemistry (19-10-2007)“…A member of the M18 family of aspartyl aminopeptidases is expressed by all intra-erythrocytic stages of the human malaria parasite Plasmodium falciparum…”
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A synthetic method for diversification of the P1′ substituent in phosphinic dipeptides as a tool for exploration of the specificity of the S1′ binding pockets of leucine aminopeptidases
Published in Bioorganic & medicinal chemistry (01-05-2007)“…A novel, general, and versatile method of diversification of the P1′ position in phosphinic pseudodipeptides, presumable inhibitors of proteolytic enzymes, was…”
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Remarkable Potential of the α-Aminophosphonate/Phosphinate Structural Motif in Medicinal Chemistry
Published in Journal of medicinal chemistry (08-09-2011)Get full text
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Peptide and Pseudopeptide Bond Synthesis in Phosphorus Dipeptide Analogs
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2020)“…Peptide analogs modified with a phosphorus-based moiety (phosphonate, phosphonamidate, or phosphinate) have emerged as invaluable tools in fundamental and…”
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