Výsledky vyhledávání - "Gordon Bruton"

Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight ‘molecular budget’

Autor: Nigel Deeks, Torquil I. Jack, Jonathan D. Goodacre, Martin Sims, Nigel J. Parr, Martin Brandt, Pamela Thomas, Kevin R. Page, Gordon Bruton, James H. Thorpe, Afjal Hussain Miah, Lena Shukla, Duncan S. Holmes, Matthew J Lindon, Leanne Cutler, Erica Christodoulou, David Jonathan Hirst

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 30:127533

Structure-based led optimisation of orally active reversible Methionine Aminopeptidase-2 (MetAP-2) inhibitors utilising a 'molecular budget' medicinal chemistry strategy is described. The key physicochemical parameters of target molecules (cLogP, mol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::93cb2e3ab05c206d81698d96ed138dcc
https://doi.org/10.1016/j.bmcl.2020.127533

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Identifying Small-Molecule Binding Sites for Epigenetic Proteins at Domain-Domain Interfaces

Autor: David, Bowkett, Romain, Talon, Cynthia, Tallant, Chris, Schofield, Frank, von Delft, Stefan, Knapp, Gordon, Bruton, Paul E, Brennan

Publikováno v: ChemMedChem. 13(10)

Epigenetics is a rapidly growing field in drug discovery. Of particular interest is the role of post-translational modifications to histones and the proteins that read, write, and erase such modifications. The development of inhibitors for reader dom

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::ca176912f54a6af54e3a9eb03100c1c0
https://pubmed.ncbi.nlm.nih.gov/29578648

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C−H Insertion Approach to the Synthesis of endo,exo-Furofuranones: Synthesis of (±)-Asarinin, (±)-Epimagnolin A, and (±)-Fargesin

Autor: Jeremy D. Hinks, Richard C. D. Brown, Nigel A. Swain, Carole J. R. Bataille, Gordon Bruton

Publikováno v: The Journal of Organic Chemistry. 66:6719-6728

A series of novel 5-aryl-4-aryloxymethyl-3-diazotetrahydrofuran-2-ones (12, 24, and 35a/b) have been prepared and found to undergo regio- and stereoselective C-H insertion reactions to afford 2,6-diaryl-3,7-dioxabicyclo[3.3.0]octane-8-ones (18, 26, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a51ae0855358da06c3ea6689d46af00
https://doi.org/10.1021/jo015829q

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Penem inhibitors of bacterial signal peptidase

Autor: Mclean Sara Denise, Gerald Brooks, Terence C. Smale, Aileen Edwina Allsop, Arun C. Kaura, Peter D. Edwards, Neil D. Pearson, Robert Southgate, Gordon Bruton, Ian Keith Hatton, Steven Coulton

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:443-448

C(3)-Penem esters and amides having the (5 S )-configuration at the bridgehead are inhibitors of Escherichia coli leader peptidase, the best activity being seen with a 6-(1-acetoxyethyl) derivative having the (5 S , 6 S , 8 R )-stereochemistry. These

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0904198aa981fd696520ef6f58742e7d
https://doi.org/10.1016/0960-894x(95)00052-u

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Tricyclic bridged β-lactams as transition state analogues: a study using semi-empirical molecular orbital methods

Autor: Gordon Bruton

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:2329-2332

The effect of ring strain on nitrogen pyramidality and carboxylate orientation was measured for six novel β-lactam nuclei using both the AM1 and PM3 methods within MOPAC. Comparison with X-ray data resulted in novel carba -cephem and -penem nuclei b

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::66206afcdc4b397bcf5c0c5b59ac2054
https://doi.org/10.1016/s0960-894x(01)80949-5

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