Search Results - "ILEY, Jim"

New insights on repellent recognition by Anopheles gambiae odorant-binding protein 1 by Tzotzos, George, Iley, Jim N, Moore, Elaine A

“…It is generally recognized that insect odorant binding proteins (OBPs) mediate the solubilisation and transport of hydrophobic odorant molecules and contribute…”
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The 1,4-naphthoquinone scaffold in the design of cysteine protease inhibitors by Valente, Cláudia, Moreira, Rui, Guedes, Rita C., Iley, Jim, Jaffar, Mohammed, Douglas, Kenneth T.

“…1,4-Naphthoquinone derivatives were found to be irreversible inhibitors for papain and bovine spleen cathepsin B. The chemical reactivity of the compounds…”
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Structure-activity Studies of the Binding of the Flavonoid Scaffold to DNA by RAGAZZON, Patricia A, ILEY, Jim, MISSAILIDIS, Sotiris

“…Background: Flavonoids have been shown to have a wide variety of biological activities and proven to be good scaffolds for the design of DNA-binding agents as…”
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The Characterisation of Flavone-DNA Isoform Interactions as a Basis for Anticancer Drug Development by RAGAZZON, Patricia A, BRADSHAW, Tracey, MATTHEWS, Charlie, ILEY, Jim, MISSAILIDIS, Sotiris

“…Background: The interactions of small molecules with nucleic acids are of considerable interest for the design of novel anticancer compounds. The physical…”
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Crystallization and preliminary diffraction studies of porcine pancreatic elastase in complex with a novel inhibitor by Oliveira, Tânia F, Mulchande, Jalmira, Moreira, Rui, Iley, Jim, Archer, Margarida

“…Porcine pancreatic elastase (PPE) was crystallized in complex with a novel inhibitor at pH 5 and X-ray diffraction data were collected at a synchrotron source…”
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Acyloxymethyl as a drug protecting group. Part 6 by Lopes, Francisca, Moreira, Rui, Iley, Jim

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Reaction of naphthoquinones with substituted nitromethanes. Facile synthesis and antifungal activity of naphtho[2,3- d]isoxazole-4,9-diones by Santos, Maria M.M., Faria, Natália, Iley, Jim, Coles, Simon J., Hursthouse, Michael B., Martins, M. Luz, Moreira, Rui

“…We report here a simple entry into naphtho[2,3- d]isoxazole-4,9-dione system containing a EWG in position 3 using the readily available…”
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4-Oxo-β-lactams (Azetidine-2,4-diones) Are Potent and Selective Inhibitors of Human Leukocyte Elastase by Mulchande, Jalmira, Oliveira, Rudi, Carrasco, Marta, Gouveia, Luís, Guedes, Rita C, Iley, Jim, Moreira, Rui

“…Human leukocyte elastase (HLE) is a serine protease stored in and secreted from neutrophils that plays a determinant role in the pathogenesis of several lung…”
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A carbamate-based approach to primaquine prodrugs: Antimalarial activity, chemical stability and enzymatic activation by Mata, Graça, do Rosário, Virgílio E., Iley, Jim, Constantino, Luís, Moreira, Rui

“…O-Alkyl carbamate derivatives of primaquine were shown to display potent transmission-blocking antimalarial activity. O-Alkyl and O-aryl carbamate derivatives…”
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Dipeptide vinyl sultams: Synthesis via the Wittig–Horner reaction and activity against papain, falcipain-2 and Plasmodium falciparum by Valente, Cláudia, Guedes, Rita C., Moreira, Rui, Iley, Jim, Gut, Jiri, Rosenthal, Philip J.

“…Vinyl sultams were prepared via the Wittig–Horner reaction and revealed to be active against recombinant falcipain-2 and Plasmodium falciparum W2. The…”
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Towards an efficient prodrug of the alkylating metabolite monomethyltriazene: Synthesis and stability of N-acylamino acid derivatives of triazenes by Perry, Maria de Jesus, Carvalho, Emília, Rosa, Eduarda, Iley, Jim

“…A series of 3-[α-(acylamino)acyl]-1-aryl-3-methyltriazenes 6a– l, potential cytotoxic triazene prodrugs, were synthesised by coupling 1-aryl-3-methyltriazenes…”
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A carbamate-based approach to primaquine prodrugs: Antimalarial activity, chemical stability and enzymatic activation: Symposium-in-Print: Chemical Proteomics by MATA, Graça, DO ROSARIO, Virgílio E, ILEY, Jim, CONSTANTINO, Luis, MOREIRA, Rui

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Azetidine-2,4-diones (4-Oxo-β-lactams) as Scaffolds for Designing Elastase Inhibitors by Mulchande, Jalmira, Guedes, Rita C, Tsang, Wing-Yin, Page, Michael I, Moreira, Rui, Iley, Jim

“…A new class of inhibitors 4-oxo-β-lactams (azetidine-2,4-diones), containing the required structural elements for molecular recognition, inhibit porcine…”
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Basic hydrolysis of quinolinyl N,N-dimethylcarbamates: a two-step mechanism by Silva, Daniel, Norberto, Fátima, Santos, Susana, Iley, Jim

“…The reactivity of 6‐quinolinyl and 8‐quinolinyl N,N‐dimethylcarbamates was examined in several aqueous basic media. A quadratic dependence was observed for the…”
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Imidazolidin-4-one Derivatives of Primaquine as Novel Transmission-Blocking Antimalarials by Araújo, Maria João, Bom, Joana, Capela, Rita, Casimiro, Catarina, Chambel, Paula, Gomes, Paula, Iley, Jim, Lopes, Francisca, Morais, José, Moreira, Rui, de Oliveira, Eliandre, do Rosário, Virgílio, Vale, Nuno

“…Imidazolidin-4-one derivatives of primaquine were synthesized as potential double prodrugs of the parent drug. The title compounds inhibit the development of…”
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Towards an efficient prodmg of the alkylating metabolite monomethyltriazene : Synthesis and stability of N-acylamino acid derivatives of triazenes by PERRY, Maria De Jesus, CARVALHO, Emilia, ROSA, Eduarda, ILEY, Jim

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Synthesis of imidazolidin-4-one and 1H-imidazo[2,1-a]isoindole-2,5(3H,9bH)-dione derivatives of primaquine: scope and limitations by Gomes, Paula, Araújo, Maria João, Rodrigues, Manuela, Vale, Nuno, Azevedo, Zélia, Iley, Jim, Chambel, Paula, Morais, José, Moreira, Rui

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N-Acyl and N-sulfonyloxazolidine-2,4-diones are pseudo-irreversible inhibitors of serine proteases by Santana, Ana Bela, Lucas, Susana D., Gonçalves, Lídia M., Correia, Henrique F., Cardote, Teresa A.F., Guedes, Rita C., Iley, Jim, Moreira, Rui

“…The synthesis, inhibitory activity and mode of action of oxazolidine-2,4-diones against porcine pancreatic elastase, here used as a model for human neutrophil…”
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Dopamine- and tyramine-based derivatives of triazenes: Activation by tyrosinase and implications for prodrug design by Perry, M. Jesus, Mendes, Eduarda, Simplício, Ana Luísa, Coelho, Ana, Soares, Ricardo V., Iley, Jim, Moreira, Rui, Francisco, Ana Paula

“…A range of triazene derivatives were synthesized and investigated as prodrug candidates for melanocyte-directed enzyme prodrug therapy (MDEPT). The prodrugs…”
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Reactivity of imidazolidin-4-one derivatives of primaquine: implications for prodrug design by Chambel, Paula, Capela, Rita, Lopes, Francisca, Iley, Jim, Morais, José, Gouveia, Luís, Gomes, José R.B., Gomes, Paula, Moreira, Rui

“…In contrast to peptide-based imidazolidin-4-ones, those synthesized from N-(α-aminoacyl) derivatives of the antimalarial drug, primaquine and ketones are…”
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