Lead Optimization for Medicinal Chemists: Pharmacokinetic Properties of Functional Groups and Organic Compounds

Front Cover
John Wiley & Sons, May 21, 2012 - Science - 622 pages
Small structural modifications can significantly affect the pharmacokinetic properties of drug candidates. This book, written by a medicinal chemist for medicinal chemists, is a comprehensive guide to the pharmacokinetic impact of functional groups, the pharmacokinetic optimization of drug leads, and an exhaustive collection of pharmacokinetic data, arranged according to the structure of the drug, not its target or indication. The historical origins of most drug classes and general aspects of modern drug discovery and development are also discussed. The index contains all the drug names and synonyms to facilitate the location of any drug or functional group in the book.
This compact working guide provides a wealth of information on the ways small structural modifications affect the pharmacokinetic properties of organic compounds, and offers plentiful, fact-based inspiration for the development of new drugs. This book is mainly aimed at medicinal chemists, but may also be of interest to graduate students in chemical or pharmaceutical sciences, preparing themselves for a job in the pharmaceutical industry, and to healthcare professionals in need of pharmacokinetic data.
 

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Contents

The Drug Discovery Process
3
Lead Optimization
13
10
29
56
36
Arenes
45
7
58
Phenols
82
Ethers
91
Thiocarbonyl Compounds
201
Phosphoric Acid Derivatives
213
1
240
65
251
67
257
Phenethylamines2Phenylethylamines
267
68
274
Aminoalkylindoles and Indole Alkaloids
291

Peroxides
97
Sulfoxides
104
1
116
Quaternary Ammonium Salts
118
61
132
Anilines
133
Aldehydes
138
62
140
63
149
Carboxylic Esters
164
Nitriles
184
Dibenzazepines and Related Tricyclic Compounds
310
Opiates
329
Peptides Peptidomimetics and Related Oligoamides
347
1
365
References
477
Quinolonecarboxylic Acids Gyrase Inhibitors
514
Prostaglandin Analogs
538
Folic Acid Analogs Antifolates
551
497
567
Copyright

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About the author (2012)

Florencio Zaragoza Dörwald studied chemistry at the Georg-August University in Göttingen, Germany, and Université LouisPasteur, Strasbourg, France, where he obtained his Ph.D. in 1990 on the synthesis of natural products under the guidance of M. Franck-Neumann and M. Miesch. He spent one postdoctoral year in both the groups of A. Pfaltz (University of Basel) and A. P. Marchand (University of North Texas), and then worked on the synthesis of unnatural amino acids at the Technical University of Dresden. From 1994 to 2007 he had a position as a medicinal chemist at Novo Nordisk A/S, Denmark. Currently, he is employed as organic chemist at Lonza AG in Visp, Switzerland.

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