Molecular hybridization yields triazole bronchodilators for the treatment of COPD

Autor: Emilio F. Stuart, Nick Clarke, Paul Alan Glossop, Neil Feeder, Strang Ross Sinclair, J. W. Watson, Jane L. Burrows, Amy S. Kenyon, Matthew D. Selby, Michael A. Trevethick, Sheena Patel, Rhys M. Jones, Kim James, Karen N. Wright, Dannielle Frances Roberts, Lyn H. Jones

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 25:5121-5126

A 1,2,4-triazole motif was employed as a bioisostere for the ester commonly used in muscarinic antagonists, and subsequent integrative conjugation to a β2 agonist quinolinone furnished a new class of bifunctional MABAs for the treatment of COPD. Med

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d1b09018de8f7e915b91637ee9153193
https://doi.org/10.1016/j.bmcl.2015.10.008

The Claisen rearrangement approach to fused bicyclic medium-ring oxacycles

Autor: Paul T. O'Sullivan, John E. Davies, Ian Collins, Neil Feeder, Andrew D. Bond, Andrew B. Holmes, Jonathan W. Burton, Edward A. Anderson

Publikováno v: Burton, J, Anderson, E, O'Sullivan, P, Collins, I, Davies, J, Bond, A, Feeder, N & Holmes, A 2008, ' The Claisen rearrangement approach to fused bicyclic medium-ring oxacycles ', Organic & Biomolecular Chemistry, vol. 6, pp. 693-702 . https://doi.org/10.1039/b715354f

The synthesis of five fused-bicyclic medium-ring lactones carrying identical ring-fusion to that in the polyether toxins is described using an enolate hydroxylation, intramolecular hydrosilation, Claisen rearrangement sequence.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2bc6a975d6e1425df4ef46a081a4fbc8
https://doi.org/10.1039/b715354f

H-bond competition experiments in solution and the solid state

Autor: James McKenzie, Christopher A. Hunter, Neil Feeder

The H-bonding outcomes in crystal structures of simple molecules, where two potential H-bonds can be formed, have been used to calculate relative H-bond probabilities for 59 combinations of H-bond donors and H-bond acceptors. H-bond probabilities are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::768d5bdbf5a31f2ad9761ff77c9e4719
https://www.repository.cam.ac.uk/handle/1810/252859

Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a ‘magic methyl’ giving a 35-fold improvement in binding

Autor: Yogesh A. Sabnis, Alan John Pettman, Bernard Joseph Banks, Neil Feeder, Robert Crook, Graham Lunn

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 21:4608-4611

In looking for a novel achiral μ opioid receptor antagonist for the treatment of pruritus, we designed and synthesised azabicyclo[3.1.0]hexane compounds as a new class of opioid ligand. During optimisation, an addition of a single methyl resulted in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a0e297263a99c7bdbaee7eefac415c3a
https://doi.org/10.1016/j.bmcl.2011.05.132

Hydrogen-bond motifs in the crystals of hydrophobic amino acids

Autor: James A. Chisholm, W. D. Samuel Motherwell, László Fábián, Peter T. A. Galek, Neil Feeder

Publikováno v: Acta Crystallographica Section B Structural Science. 64:504-514

A computer program has been developed to survey a set of crystal structures for hydrogen-bond motifs. Possible ring and chain motifs are generated automatically from a user-defined list of interacting molecular fragments and intermolecular interactio

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4a2ee0650e74e5a1622a261b5c383639
https://doi.org/10.1107/s0108768108019149