Analogue-Based Drug Discovery III by Janos Fischer, C. Robin Ganellin, David P. Rotella

By Janos Fischer, C. Robin Ganellin, David P. Rotella

Such a lot medicines are analogue medications. There are not any basic ideas how a brand new drug may be chanced on, however, there are a few observations which aid to discover a brand new drug, and in addition somebody tale of a drug discovery can start up and aid new discoveries. quantity III is a continuation of the profitable e-book sequence with new examples of tested and lately brought medicinal drugs.
the foremost a part of the ebook is written by means of key inventors both as a case research or a research of an analogue type. With its wide variety throughout quite a few healing fields and chemical sessions, this is often of curiosity to almost each researcher in drug discovery and pharmaceutical chemistry, and -- including the former volumes -- constitutes the 1st systematic method of drug analogue development.Content:
Chapter 1 Pioneer and Analogue medications (pages 1–19): Prof. Dr. Janos Fischer, Prof. Dr. C. Robin Ganellin and Prof. Dr. David P. Rotella
Chapter 2 pageant within the Pharmaceutical Drug improvement (pages 21–35): Christian Tyrchan and Fabrizio Giordanetto
Chapter three Metabolic balance and Analogue?Based Drug Discovery (pages 37–75): Amit S. Kalgutkar and Antonia F. Stepan
Chapter four Use of Macrocycles in Drug layout Exemplified with Ulimorelin, a possible Ghrelin Agonist for Gastrointestinal Motility problems (pages 77–110): Dr. Mark L. Peterson, Dr. Hamid Hoveyda, Dr. Graeme Fraser, Eric Marsault and Rene Gagnon
Chapter five the invention of Anticancer medicines focusing on Epigenetic Enzymes (pages 111–139): A. Ganesan
Chapter 6 Thienopyridyl and Direct?Acting P2Y12 Receptor Antagonist Antiplatelet medicines (pages 141–164): Dr. Joseph A. Jakubowski and Atsuhiro Sugidachi
Chapter 7 Selective Estrogen Receptor Modulators (pages 165–185): Amarjit Luniwal, Rachael Jetson and Paul Erhardt
Chapter eight Discovery of Nonpeptide Vasopressin V2 Receptor Antagonists (pages 187–209): Kazumi Kondo and Hidenori Ogawa
Chapter nine the advance of Cysteinyl Leukotriene Receptor Antagonists (pages 211–239): Peter R. Bernstein
Chapter 10 the invention of Dabigatran Etexilate (pages 241–267): Norbert Hauel, Andreas Clemens, Herbert Nar, Henning Priepke, Joanne van Ryn and Wolfgang Wienen
Chapter eleven the invention of Citalopram and Its Refinement to Escitalopram (pages 269–294): Klaus P. Bogeso and Connie Sanchez
Chapter 12 Tapentadol – From Morphine and Tramadol to the invention of Tapentadol (pages 295–318): Helmut Buschmann
Chapter thirteen Novel Taxanes: Cabazitaxel Case research (pages 319–341): Dr. Herve Bouchard, Dr. Dorothee Semiond, Dr. Marie?Laure Risse and Dr. Patricia Vrignaud
Chapter 14 Discovery of Boceprevir and Narlaprevir: A Case learn for function of Structure?Based Drug layout (pages 343–363): Srikanth Venkatraman, Andrew Prongay and George F. Njoroge
Chapter 15 A New?Generation Uric Acid creation Inhibitor: Febuxostat (pages 365–376): Ken Okamoto, Shiro Kondo and Takeshi Nishino

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Med. , 46, 2774–2789. -U. and Mattei, P. (2010) Dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes, in AnalogueBased Drug Discovery II (eds J. R. Ganellin), Wiley-VCH Verlag GmbH, Weinheim, pp. 109–134. , and Fareed, J. (1999) Pharmacology of argatroban. Expert Opin. Invest. Drugs, 8 (5), 625–654. Gustafsson, D. and Elg, M. (2003) The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review.

Drugs, 8 (5), 625–654. Gustafsson, D. and Elg, M. (2003) The pharmacodynamics and pharmacokinetics of the oral direct thrombin inhibitor ximelagatran and its active metabolite melagatran: a mini-review. Thromb. , 109 (Suppl. 1), S9–S15. , Lewis, J. , and Shet, S. (2005) Hepatic findings in long-term clinical trials of ximelagatran. , 28 (4), 351–370. , and Wienen, W. (2002) Structure-based design of novel potent nonpeptide thrombin inhibitors. J. Med. , 45, 1757–1766. W. I. (2010) Update on antithrombotic therapy.

In this scenario, the electron-withdrawing effects of the fluorine atom most likely rendered the phenyl group resistant to CYP oxidation. 5) [11]. ADME profiling of 14 revealed a short metabolic half-life in HLM and rat liver microsomes, which was consistent with rapid clearance in rats. Metabolite identification studies indicated extensive hydroxylation on the pendant phenyl groups of the benzhydryl motif, which led to the design of the corresponding bis-(4-fluorophenyl) analogue 15 in order to block the metabolically vulnerable sites with fluorine atoms.

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