Výsledky vyhledávání - "Nigel J. P. Broom"

Rational Design of Femtomolar Inhibitors of Isoleucyl tRNA Synthetase from a Binding Model for Pseudomonic Acid-A

Autor: Michael L. Doyle, Peter J. O'Hanlon, Lucy Mensah, Andrew Keith Forrest, Christine M. Richardson, Murray J. B. Brown, Andrew J. Pope, Nigel J. P. Broom, Neal Osbourne

Publikováno v: Biochemistry. 39:6003-6011

This paper describes the design and characterization of novel inhibitors of IleRS, whose binding affinity approaches the tightest reported for noncovalent inhibition. Compounds were designed from a binding model for the natural product pseudomonic ac

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bd6ce0b9973957635c392291f7c2812
https://doi.org/10.1021/bi000148v

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Synthesis and antibacterial properties of β-diketone acrylate bioisosteres of pseudomonic acid A

Autor: Nigel J. P. Broom, John Stephen Elder, Nicky D. Masson, Isobel Bennett, Robert Cassels, Peter J. O'Hanlon

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 9:1847-1852

A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 have been synthesized and evaluated for their ability to inhibit bacterial isoleucyl-tRNA synthetase and act as antibacterial agents. A number of analogues have excellent antib

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d0bd12d52c61bcbbe24ba7765ed82dcc
https://doi.org/10.1016/s0960-894x(99)00296-6

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Characterization of Isoleucyl-tRNA Synthetase from Staphylococcus aureus

Autor: Neil Benson, Lucy Mensah, Andrew J. Pope, Keith J. Moore, Mary McVey, Murray J. B. Brown, Neal Osbourne, Nigel J. P. Broom, Peter J. O'Hanlon

Publikováno v: Journal of Biological Chemistry. 273:31691-31701

The interactions of isoleucyl-tRNA synthetase (IleRS, E) from Staphylococcus aureus with both intermediate analogues and pseudomonic acid (PS-A) have been investigated using transient and steady-state techniques. Non-hydrolyzable analogues of isoleuc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e2ab739d2b57c422fdc2a3ec6950b404
https://doi.org/10.1074/jbc.273.48.31691

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The Chemistry of Pseudomonic Acid. 18. Heterocyclic Replacement of the α,β-Unsaturated Ester: Synthesis, Molecular Modeling, and Antibacterial Activity

Autor: Neal Frederick Osborne, J. M. Wilson, Timothy J. Mitchell, Nigel J. P. Broom, Peter J. O'Hanlon, Desmond John Best, Pamela Brown, Robert Cassels

Publikováno v: Journal of Medicinal Chemistry. 40:2563-2570

The electronic requirements around the C1-C3 region of pseudomonic acid analogues were investigated. Synthetic routes were developed to access a range of compounds where the alpha, beta-unsaturated ester moiety had been replaced by a 5-membered ring

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86c8c0a6f0b463ead739c168eb169393
https://doi.org/10.1021/jm960738k

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Chemistry of Pseudomonic Acid. Part 16. Aryl and Heteroaryl Ketone Derivatives of Monic Acid

Autor: J. M. Wilson, Andrew Keith Forrest, John Stephen Elder, Neil D. Pearson, Philippa A. Coates, Angela Abson, Nicky D. Masson, Peter J. O'Hanlon, Nigel J. P. Broom, Amanda J. Hicks, Peter Charles Thomas Hannan, J. E. Pons

Publikováno v: The Journal of Antibiotics. 49:390-394

The synthesis, antibacterial activities, murine pharmacokinetic and infection model data for a range of aryl and heteroaryl ketone derivatives of monic acid (2a) are reported. The best results were found for the 3-furyl and 2-methoxy thiazol-5-yl ana

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d863a8b406d31ac36f85500de969a4d
https://doi.org/10.7164/antibiotics.49.390

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The Chemistry of Pseudomonic Acid. Part 14. Synthesis and In Vivo Biological Activity of Heterocyclyl Substituted Oxazole Derivatives

Autor: Peter J. O'hanlon, Graham Walker, John S. Elder, J. M. Wilson, Peter Charles Thomas Hannan, P. Woodall, J. E. Pons, Nigel J. P. Broom

Publikováno v: The Journal of Antibiotics. 48:1336-1344

Semisynthetic analogues of pseudomonic acid A have been prepared containing a heterocyclyl substituted oxazole. Derivatives in which the heterocycle was thiophene, furan, pyridine, or isoxazole showed good antibacterial potency and were further evalu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5308d863d553428d384d316d468ebcba
https://doi.org/10.7164/antibiotics.48.1336

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Preparation of E-(2-substituted-1-methylethylidene)indanones derived from monic acid

Autor: Peter J. O'Hanlon, Nigel J. P. Broom, Neil D. Pearson

Publikováno v: Tetrahedron Letters. 35:3771-3774

Alkylation of the lithium dienolate of the monic acid hydroxamate (3) with o-bromo(bromomethyl) benzene or heteroaromatic derivatives gave α-alkylated products (5). This alkylation procedure was surprisingly catalysed by 4-dimethylaminopyridine. Met

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https://doi.org/10.1016/s0040-4039(00)73095-4

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Synthesis of (5R)-(Z)-6-(1-methyl-1,2,3-triazol-4-ylmethylene)penem-3-carboxylic acid, a potent broad spectrum β-lactamase inhibitor, from 6-aminopenicillanic acid

Autor: John Barry Harbridge, Nigel J. P. Broom, Graham Walker, Richard J. Atkins, Steven Coulton, Neal Frederick Osborne, Irene Stirling-François, Michael Anthony Harris

Publikováno v: J. Chem. Soc., Perkin Trans. 1. :179-188

(5R)-(Z)-6-(1-Methyl-1,2,3-triazol-4-ylmethylene)penem-3-carboxylic acid 34(BRL 42715) has been prepared from 6-aminopenicillanic acid 4(6-APA) by a short, stereoselective and efficient route via the novel intermediate, p-methoxybenzyl (5R, 6S)-6-bro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::91e0769f511a7a6201960eac2e50ce4a
https://doi.org/10.1039/p19940000179

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ChemInform Abstract: Synthesis of (5R)-(Z)-6-(1-Methyl-1,2,3-triazol-4-ylmethylene)penem-3- carboxylic Acid, a Potent Broad Spectrum β-Lactamase Inhibitor, from 6-Aminopenicillanic Acid

Autor: Irene Stirling-François, Neal Frederick Osborne, Graham Walker, Richard J. Atkins, John Barry Harbridge, Michael Anthony Harris, Steven Coulton, Nigel J. P. Broom

Publikováno v: ChemInform. 25

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::910a06cc89341ac6c8679ec74eed2bb5
https://doi.org/10.1002/chin.199418247

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