N
Neal Frederick Osborne
Researcher at Pfizer
Publications - 21
Citations - 2061
Neal Frederick Osborne is an academic researcher from Pfizer. The author has contributed to research in topics: Carboxylic acid & Reductive elimination. The author has an hindex of 13, co-authored 21 publications receiving 2028 citations.
Papers
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Burger's medicinal chemistry and drug discovery
Manfred E. Wolff,William Foye,Robert Southgate,Neal Frederick Osborne,Michael J. Pearson,George Burton,SmithKline Beecham +6 more
Journal ArticleDOI
The chemistry of pseudomonic acid. 18. Heterocyclic replacement of the alpha,beta-unsaturated ester: synthesis, molecular modeling, and antibacterial activity.
Pamela Brown,Desmond John Best,Nigel J. P. Broom,Robert Cassels,Peter J. O'Hanlon,Timothy J. Mitchell,Neal Frederick Osborne,J. M. Wilson +7 more
TL;DR: The electronic requirements around the C1-C3 region of pseudomonic acid analogues were investigated and synthetic routes were developed to access a range of compounds where the alpha, beta-unsaturated ester moiety had been replaced by a 5-membered ring heterocycle.
Journal ArticleDOI
Molecular recognition of tyrosinyl adenylate analogues by prokaryotic tyrosyl tRNA synthetases.
Pamela Brown,Christine M. Richardson,Lucy Mensah,Peter J. O'Hanlon,Neal Frederick Osborne,Andrew J. Pope,Graham Walker +6 more
TL;DR: Micromolar and sub-micromolar inhibitors of tyrosyl tRNA synthetases from both B. stearothermophilus and Staphylococcus aureus have been synthesised and the importance of the adenine ring to the binding of tyrosinyl adenylate to the enzyme has been highlighted.
Journal ArticleDOI
6-(substituted methylene)penems, potent broad spectrum inhibitors of bacterial beta-lactamase. III. Structure-activity relationships of the 5-membered heterocyclic derivatives.
Isabel S. Bennett,Nigel J. P. Broom,G. Bruton,S. Calvert,B. P. Clarke,Kenneth Coleman,R. Edmondson,Peter D. Edwards,D. Jones,Neal Frederick Osborne,Graham Walker +10 more
TL;DR: Sodium (5RS)-Z-6-(heterocyclylmethylene)penem-3-carboxylates (2) are a series of extremely potent inhibitors of bacterial beta-lactamases as mentioned in this paper.
Journal ArticleDOI
A novel and stereocontrolled synthesis of (5R)-(Z)-6-(1-methyl-1,2,3-triazol-4-ylmethylene)penem-3-carboxylic acid, a potent broad spectrum β-lactamase inhibitor
Neal Frederick Osborne,Nigel J. P. Broom,Steven Coulton,John Barry Harbridge,Michael A. Harris,Irene Stirling-François,Graham Walker +6 more
TL;DR: The key step in the preparation of the title compound (BRL 42715) from 6-aminopenicillanic acid was the condensation of the anion, generated by deprotonation of p-methoxybenzyl (5R,6S)-6-bromopenem-3-carboxylate(10), with 1-methyl-1,2,3-triazole-4-carbaldehyde; in situ acylation, followed by reductive elimination afforded the isomeric (Z)- and (E)-