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Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780123809025, 9780123809032

Annual Reports in Medicinal Chemistry, Volume 45

1st Edition

Series Editor: John Macor
Paperback ISBN: 9780123809025
eBook ISBN: 9780123809032
Imprint: Academic Press
Published Date: 25th October 2010
Page Count: 648
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Table of Contents

Section I: Central Nervous System Diseases – ROBICHAUD

  1. Voltage-Gated Calcium Channel Antagonists for the Central Nervous System
  2. James C. Barrow and Joseph L. Duffy

  3. Recent Developments in Glycine Transporter-1 Inhibitors
  4. Christopher L. Cioffi, Shuang Liu and Mark A.Wolf

  5. Modulators of Transient Receptor Potential Ion Channels
  6. Rajagopal Bakthavatchalam and S. David Kimball

  7. Defining Neuropharmacokinetic Parameters in CNS Drug Discovery to Determine Cross-species Pharmacologic Exposure-Response Relationships
  8. Christopher L. Shaffer

    Section II: Cardiovascular and Metabolic Diseases - STAMFORD

  9. High Affinity Niacin Receptor GPR109A Agonists
  10. Hong C. Shen and Steven L. Colletti

  11. Recent Advances in Acetyl CoA Carboxylase (ACC) Inhibitors
  12. Matthew P. Bourbeau, John G. Allen, and Wei Gu

  13. Enzymatic Targets in the Triglyceride Synthesis Pathway
  14. Dmitry O. Koltun and Jeff Zablocki

  15. Inhibitors of HIF Prolyl Hydroxylases
  16. Michael H. Rabinowitz, Terrance D. Barrett, Mark D. Rosen, Hariharan Venkatesan

    Section III: Inflammation / Pulmonary / GI - BARRISH/Weinstein

  17. Opioid Receptor Antagonists for Gastrointestinal Dysfunction
  18. R. William Hipkin and Roland E. Dolle

  19. CFTR Modulators for the Treatment of Cystic Fibrosis
  20. Sabine Hadida, Frederick Van Goor and Peter D. J. Grootenhuis

  21. Targeting B-cells in inflammatory disease
  22. Kevin S. Currie

  23. Modulators of Toll-Like Receptor (TLR) Signaling
  24. Mark Spyvee, Lynn Hawkins, and Sally Ishizaka

    Section IV: Oncology - McAlpine

  25. Janus Kinase 2 (JAK2) inhibitors for the treatment of myeloproliferative neoplasm (MPN)
  26. Ashok V. Purandare, Matthew V. Lorenzi and Louis J. Lombardo

  27. Development of poly(ADP-ribose)polymerase (PARP) inhibitors in oncology
  28. Philip Jones

  29. Epigenetic Targets and Cancer Drug Discovery
  30. Patrick M. Woster, Ph.D

    Section V: Infectious Diseases - Primeau

  31. HIV-1 Integrase Strand Transfer Inhibitors
  32. Brian A. Johns

  33. Recent Advances in Drug Discovery for Neglected Tropical Diseases Caused by Infective Kinetoplastid Parasites
  34. Robert T. Jacobs and Charles Ding

  35. Recent Advances in the Inhibition of Bacterial Fatty Acid Biosynthesis
  36. Vincent Gerusz

    Section VI: Topics in Biology - LOWE

  37. Back to the Plaque: Emerging Studies That Re-Focus Attention on the Neuritic Plaque in Alzheimer’s Disease
  38. Dr. Robert B. Nelson

  39. Targeting Methyl Lysine
  40. Stephen V. Frye, Tom Heightman and Jian Jin

  41. Chemical Proteomic Technologies for Drug Target Identification
  42. Kieran F. Geoghegan and Douglas S. Johnson

  43. NIH Translational Programs for Assisting Pre-Clinical Drug Discovery and Development
  44. Raj N. Misra

    Section VII: Topics in Drug Design and Discovery - DESAI

  45. Role of Physicochemical Properties and Lipophilic Ligand Efficiency (LipE or LLE) in addressing Drug Safety Risks
  46. Martin P. Edwards and David A. Price

  47. Reducing the Risk of Drug Attrition Associated with Physicochemical Properties
  48. Paul D. Leeson and James R. Empfield

  49. Compound Collection Enhancement and Paradigms for High Throughput Screening - an Update
  50. Stevan W Djuric, Irini Akritopoulou-Zanze, Philip B Cox and Scott Galasinski

  51. The Role of Fluorine in the Discovery and Optimization of CNS Agents: Modulation of Drug-Like Properties
  52. Kevin J. Hodgetts, Kerry J. Combs, Amy M. Elder and Geraldine C. Harriman

  53. Patents in Drug Discovery: Case Studies, Examples, and Simple Steps Medicinal Chemists Can Take to Protect Hard-Won Intellectual Property
  54. Charles J. Andres, Jr. and Richard L. Treanor

    Section VIII: Trends and Perspectives

  55. To Market, To Market – 2009

Shridhar Hegde and Michelle Schmidt


Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

Key Features

  • Covers findings related to cardiovascular, inflammation, and pulmonary diseases
  • Examines issues in oncology, from mTor inhibitors to drug targets
  • Incorporates up-to-date information on drug design and discovery, including delivery to market


medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2010
25th October 2010
Academic Press
Paperback ISBN:
eBook ISBN:

Ratings and Reviews

About the Series Editor

John Macor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA