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Ilaria Giordano
Researcher at GlaxoSmithKline
Publications - 17
Citations - 1124
Ilaria Giordano is an academic researcher from GlaxoSmithKline. The author has contributed to research in topics: Type II topoisomerase & Mode of action. The author has an hindex of 13, co-authored 17 publications receiving 934 citations. Previous affiliations of Ilaria Giordano include Anacor Pharmaceuticals Inc..
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Journal ArticleDOI
Type IIA topoisomerase inhibition by a new class of antibacterial agents.
Benjamin D. Bax,Pan F. Chan,Drake S. Eggleston,Drake S. Eggleston,Andrew P. Fosberry,Daniel R. Gentry,Fabrice Gorrec,Fabrice Gorrec,Ilaria Giordano,Michael M. Hann,Alan Joseph Hennessy,Martin Hibbs,Jianzhong Huang,Emma J. Jones,Jo J. Jones,Kristin K. Brown,Ceri J. Lewis,Earl May,Earl May,Martin R. Saunders,Onkar M. P. Singh,Claus Spitzfaden,Carol Shen,Anthony Shillings,Andrew J. Theobald,Alexandre Wohlkonig,Alexandre Wohlkonig,Neil D. Pearson,Michael N. Gwynn +28 more
TL;DR: This work provides new insights into the mechanism of topoisomerase action and a platform for structure-based drug design of a new class of antibacterial agents against a clinically proven, but conformationally flexible, enzyme class.
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Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656)
Xianfeng Li,Vincent Hernandez,Fernando Rock,Wai Choi,Yvonne Mak,Manisha Mohan,Weimin Mao,Yasheen Zhou,Eric E. Easom,Jacob J. Plattner,Wuxin Zou,Esther Pérez-Herrán,Ilaria Giordano,Alfonso Mendoza-Losana,Carlos Alemparte,Joaquín Rullas,Iñigo Angulo-Barturen,Sabrinia D. Crouch,Fátima Ortega,David Barros,M. R. K. Alley +20 more
TL;DR: GSK3036656, a novel series of 3-aminomethyl 4-halogen benzoxaboroles as Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS) inhibitors, exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads.
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N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics
Paul Bamborough,Richard Martyn Angell,Inder Bhamra,David W. Brown,James A. Bull,John A. Christopher,Anthony William James Cooper,Lynsey H. Fazal,Ilaria Giordano,Lucy Hind,Vipulkumar Kantibhai Patel,Lisa E. Ranshaw,Martin Sims,Philip Alan Skone,Smith Kathryn Jane,Emma Vickerstaff,Melanie Washington +16 more
TL;DR: 2,4-Dianilino pyrimidines are well-known inhibitors of tyrosine kinases including lymphocyte specific kinase (Lck) and structure-activity relationships at the 4-position are discussed and rationalised.
Journal ArticleDOI
Novel hydroxyl tricyclics (e.g., GSK966587) as potent inhibitors of bacterial type IIA topoisomerases
Timothy J. Miles,Alan Joseph Hennessy,Ben Bax,Gerald Brooks,Barry S. Brown,Pamela Brown,Nathalie Cailleau,Dongzhao Chen,Steven Dabbs,David T. Davies,Joel Michael Esken,Ilaria Giordano,Jennifer Hoover,Jianzhong Huang,Graham Elgin Jones,Senthill K. Kusalakumari Sukmar,Claus Spitzfaden,Roger Edward Markwell,Elisabeth A. Minthorn,Steve Rittenhouse,Michael N. Gwynn,Neil D. Pearson +21 more
TL;DR: X-ray crystallographic studies were used to provide insight into the structural basis for the difference in antibacterial potency between enantiomers and advanced studies were reported on compound 1 which demonstrates good PK and in vivo efficacy properties.
Journal ArticleDOI
Novel amino-piperidines as potent antibacterials targeting bacterial type IIA topoisomerases.
Timothy J. Miles,Jeffrey M. Axten,Christopher Barfoot,Gerald Brooks,Pamela Brown,Dongzhao Chen,Steven Dabbs,David T. Davies,David L. Downie,Susanne Eyrisch,Timothy Francis Gallagher,Ilaria Giordano,Michael N. Gwynn,Alan Joseph Hennessy,Jennifer Hoover,Jianzhong Huang,Graham Elgin Jones,Roger Edward Markwell,William H. Miller,Elizabeth A. Minthorn,Stephen Rittenhouse,Mark A. Seefeld,Neil D. Pearson +22 more
TL;DR: A series of amino-piperidine antibacterials with a good broad spectrum potency and good pharmacokinetics, broad spectrum antibacterial activity and oral efficacy in a rat lung infection model are identified.