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Dive into the research topics where Henry A. Kelly is active.

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Featured researches published by Henry A. Kelly.


Drug Discovery Today | 2013

A practical drug discovery project at the undergraduate level.

M. Jonathan Fray; Simon J. F. Macdonald; Ian Robert Baldwin; Nicholas Paul Barton; Jack A. Brown; Ian B. Campbell; Ian Churcher; Diane Mary Coe; Anthony William James Cooper; Andrew P. Craven; Gail Fisher; Graham G. A. Inglis; Henry A. Kelly; John Liddle; Aoife C. Maxwell; Vipulkumar Kantibhai Patel; Stephen Swanson; Natalie Wellaway

In this article, we describe a practical drug discovery project for third-year undergraduates. No previous knowledge of medicinal chemistry is assumed. Initial lecture workshops cover the basic principles; then students, in teams, seek to improve the profile of a weakly potent, insoluble phosphatidylinositide 3-kinase delta (PI3Kδ) inhibitor (1) through compound array design, molecular modelling, screening data analysis and the synthesis of target compounds in the laboratory. The project benefits from significant industrial support, including lectures, student mentoring and consumables. The aim is to make the learning experience as close as possible to real-life industrial situations. In total, 48 target compounds were prepared, the best of which (5b, 5j, 6b and 6ap) improved the potency and aqueous solubility of the lead compound (1) by 100-1000 fold and ≥tenfold, respectively.


Journal of Workplace Learning | 2011

Reflection in a Workplace Qualification: Challenges and Benefits.

Pauline M. Hegarty; Henry A. Kelly; Anita Walsh

Purpose – The purpose of this paper is to discuss the challenges and benefits that arose from the implementation of an innovative example of employer responsive provision, i.e. of a postgraduate programme that is work‐based and designed specifically to meet the needs of the organisation.Design/methodology/approach – The approach is to outline the principles and challenges involved in designing a postgraduate programme that combines both scientific and personal/professional development in a way that is extremely unusual. In order to achieve this, in addition to assessment of technical scientific skills, it was necessary to integrate pedagogy that would support critical reflection on wider professional practice into the programme. The use of reflection on practice adopted an approach which is not familiar to the scientific community.Findings – Adoption of reflection on practice introduced particular challenges for programme design and delivery that required those involved to review their own practice critic...


Journal of Medicinal Chemistry | 2007

Factor Xa Inhibitors: S1 Binding Interactions of a Series of N-{(3S)-1-[(1S)-1-Methyl-2-Morpholin-4-Yl-2-Oxoethyl]-2-Oxopyrrolidin-3-Yl}Sulfonamides.

Chuen Chan; Alan David Borthwick; David W. Brown; Cynthia L. Burns-Kurtis; Matthew Campbell; Laiq Chaudry; Chun-wa Chung; J. Nicole Hamblin; Lisa Johnstone; Henry A. Kelly; Savvas Kleanthous; Angela Patikis; Champa Patel; Anthony J. Pateman; Stefan Senger; Gita P. Shah; John R. Toomey; Nigel S. Watson; Helen E. Weston; Caroline Whitworth; and Robert J. Young; Ping Zhou


Bioorganic & Medicinal Chemistry Letters | 2006

Structure- and property-based design of factor Xa inhibitors: Pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs

Robert J. Young; Matthew Campbell; Alan D. Borthwick; David W. Brown; Cynthia L. Burns-Kurtis; Chuen Chan; Miriam C. Crowe; Satish Dayal; Hawa Diallo; Henry A. Kelly; N. Paul King; Savvas Kleanthous; Andrew M. Mason; Jackie E. Mordaunt; Champa Patel; Anthony J. Pateman; Stefan Senger; Gita P. Shah; Paul W. Smith; Nigel S. Watson; Helen E. Weston; Ping Zhou


Bioorganic & Medicinal Chemistry Letters | 2007

Selective and Dual Action Orally Active Inhibitors of Thrombin and Factor Xa.

Robert J. Young; David W. Brown; Cynthia L. Burns-Kurtis; Chuen Chan; Julia A. Hubbard; Henry A. Kelly; Anthony J. Pateman; Angela Patikis; Stefan Senger; Gita P. Shah; John R. Toomey; Nigel S. Watson; Ping Zhou


Bioorganic & Medicinal Chemistry Letters | 2006

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors.

Nigel S. Watson; David W. Brown; Matthew Campbell; Chuen Chan; Laiq Chaudry; Rebecca Fenwick; J. Nicole Hamblin; Claudine Haslam; Henry A. Kelly; N. Paul King; Cynthia L. Kurtis; Andrew R. Leach; Gary R. Manchee; Andrew M. Mason; Charlotte Jane Mitchell; Champa Patel; Vipulkumar Kantibhai Patel; Stefan Senger; Gita P. Shah; Helen E. Weston; Caroline Whitworth; Robert J. Young


Bioorganic & Medicinal Chemistry Letters | 2008

Structure and Property Based Design of Factor Xa Inhibitors: Pyrrolidin-2-Ones with Biaryl P4 Motifs.

Robert J. Young; Alan D. Borthwick; David W. Brown; Cynthia L. Burns-Kurtis; Matthew Campbell; Chuen Chan; Marie Charbaut; Chun-wa Chung; Henry A. Kelly; N. Paul King; Savvas Kleanthous; Andrew M. Mason; Anthony J. Pateman; Angela Patikis; Ivan Leo Pinto; Derek Pollard; Stefan Senger; Gita P. Shah; John R. Toomey; Nigel S. Watson; Helen E. Weston


Bioorganic & Medicinal Chemistry Letters | 2008

Structure and property based design of factor Xa inhibitors: biaryl pyrrolidin-2-ones incorporating basic heterocyclic motifs.

Robert J. Young; Alan D. Borthwick; David W. Brown; Cynthia L. Burns-Kurtis; Matthew Campbell; Chuen Chan; Marie Charbaut; Hawa Diallo; Eric Hortense; Wendy R. Irving; Henry A. Kelly; N. Paul King; Savvas Kleanthous; Andrew M. Mason; Anthony J. Pateman; Angela Patikis; Ivan Leo Pinto; Derek Pollard; Stefan Senger; Gita P. Shah; John R. Toomey; Nigel S. Watson; Helen E. Weston; Ping Zhou


Archive | 2004

Pyrrolidine -2-ones as factor xa inhibitors

Alan David Borthwick; Henry A. Kelly; Nigel S. Watson; Robert J. Young


Archive | 1998

Pyrrolopyrrolidine derivatives and their use as serine protease inhibitors

Steven J. Coote; Michael Dennis Dowle; Harry Finch; Michael Menteith Hann; Henry A. Kelly; Simon J. F. Macdonald; Neil Anthony Pegg; Nigel Grahame Ramsden; Nigel S. Watson

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Nigel S. Watson

University of Hertfordshire

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David W. Brown

Boston Children's Hospital

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