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The efficiency of C-4 substituents in activating the beta-lactam scaffold towards serine proteases and hydroxide ionRational design, synthesis, biophysical and antiproliferative evaluation of fluorenone derivatives with DNA G-quadruplex binding properties.N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases.Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3-d]isoxazole-4,9-diones.4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.The microsomal demethylation of N,N-dimethylbenzamides. Substituent and kinetic deuterium isotope effects.Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.Inactivation of rat liver cytochrome P450 (P450) by N,N-dimethylformamide and N,N-dimethylacetamide.Synthesis, stability and in vitro dermal evaluation of aminocarbonyloxymethyl esters as prodrugs of carboxylic acid agents.Dipeptide derivatives of primaquine as transmission-blocking antimalarials: effect of aliphatic side-chain acylation on the gametocytocidal activity and on the formation of carboxyprimaquine in rat liver homogenates.A carbamate-based approach to primaquine prodrugs: antimalarial activity, chemical stability and enzymatic activation.Imidazolidin-4-one derivatives of primaquine as novel transmission-blocking antimalarials.Kinetics and mechanism of hydrolysis of N-acyloxymethyl derivatives of azetidin-2-one.Oxidation of tertiary benzamides by 5,10,15,20-tetraphenylporphyrinatoironIII chloride-tert-butylhydroperoxide.Dopamine- and tyramine-based derivatives of triazenes: activation by tyrosinase and implications for prodrug design.Synthesis of the pyoverdin chromophore by a biomimetic oxidative cyclization.Towards an efficient prodrug of the alkylating metabolite monomethyltriazene: synthesis and stability of N-acylamino acid derivatives of triazenes.Design, synthesis, and enzymatic evaluation of N1-acyloxyalkyl- and N1-oxazolidin-2,4-dion-5-yl-substituted beta-lactams as novel inhibitors of human leukocyte elastase.Unanticipated acyloxymethylation of sumatriptan indole nitrogen atom and its implications in prodrug design.Azetidine-2,4-diones (4-oxo-beta-lactams) as scaffolds for designing elastase inhibitors.Dipeptide vinyl sultams: synthesis via the Wittig-Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum.The Bsmoc group as a novel scaffold for the design of irreversible inhibitors of cysteine proteases.Microsomal metabolism of N,N-diethyl-m-toluamide (DEET, DET): the extended network of metabolites.Cleavage of tertiary amidomethyl ester prodrugs of carboxylic acids by rat liver homogenates.Acyloxymethyl as a drug protecting group. Part 3. Tertiary O-amidomethyl esters of penicillin G: chemical hydrolysis and anti-bacterial activity.Synthesis, stability, biochemical and pharmacokinetic properties of a new potent and selective 4-oxo-β-lactam inhibitor of human leukocyte elastaseImidazolium ylides from a conjugate addition–proton transfer route and their cycloaddition reactionsCrystallization and Preliminary Diffraction Studies of Porcine Pancreatic Elastase in Complex with a Novel InhibitorThe 1,4-naphthoquinone scaffold in the design of cysteine protease inhibitorsAcyloxymethyl as a drug protecting group. Part 6Intramolecular 1,3-dipolar cycloadditions of dihydroimidazolium ylides: synthesis of pyrrolo[1,2,3-de]quinoxalines and imidazo[1,2-a]indolesPyrrolo[1,2,3-de]quinoxalines: unexpected products from 1,3-dipolar cycloaddition of dihydroimidazolium ylidesMechanism of the microsomal demethylation of 1-aryl-3,3-dimethyltriazenesAcyloxymethyl as a drug protecting group: Part 4. The hydrolysis of tertiary amidomethyl ester prodrugs of carboxylic acid agentsTriazene drug metabolites. Part 17: Synthesis and plasma hydrolysis of acyloxymethyl carbamate derivatives of antitumour triazenesTriazene drug metabolites: part 15. Synthesis and plasma hydrolysis of anticancer triazenes containing amino acid carriersPhthalimidomethyl as a drug pro-moiety. Probing its reactivityAminocarbonyloxymethyl ester prodrugs of flufenamic acid and diclofenac: suppressing the rearrangement pathway in aqueous mediaTetraplex DNA specific ligands based on the fluorenone-carboxamide scaffoldMonofluorinated di- and tetrahydropyrans via Prins-type cyclisations
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P50
description
hulumtues
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researcher
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wetenschapper
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հետազոտող
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name
Jim Iley
@ast
Jim Iley
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Jim Iley
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Jim Iley
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Jim Iley
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type
label
Jim Iley
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Jim Iley
@en
Jim Iley
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Jim Iley
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Jim Iley
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altLabel
James N Iley
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prefLabel
Jim Iley
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Jim Iley
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Jim Iley
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Jim Iley
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Jim Iley
@sl
P108
P106
P1153
7003315386
P21
P31
P496
0000-0002-2513-8159