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

  • ID: 2183403
  • Book
  • 622 Pages
  • John Wiley and Sons Ltd
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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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PART I: Introduction

THE DRUG DISCOVERY PROCESS

Pharmacokinetics –

Structure Relationship

The Future of Small–Molecule Drugs

LEAD OPTIMIZATION

What Limits/Reduces Oral Bioavailability?

What Limits/Reduces Plasma Half–Life?

How to Improve bbb–Penetration?

How to Avoid CYP Inhibition/Induction?

How to Avoid Interaction with the HumanEther–′a–go–go–Related Gene (hERG)?

How to Prevent Toxicity?

Examples of PK–Optimization in Animals

PART II: The Pharmacokinetic Properties of Compound Classes

ALKANES

Metabolism

ALKENES AND ALKYNES

Metabolism

ARENES

Metabolism

HALIDES

Fluorine

Chlorine

Bromine

Iodine

Alkylating Agents

AZIDES

NITRO COMPOUNDS

Metabolism

AZO COMPOUNDS

TRIAZENES

NITRATES AND NITRITES

N–NITROSO COMPOUNDS

N–OXIDES

ALCOHOLS

Metabolism

PHENOLS

ETHERS

Metabolism

EPOXIDES

PEROXIDES

THIOLS

THIOETHERS

Metabolism

SULFOXIDES

SULFONES

ALIPHATIC AMINES

Basicity

Metabolism

Rates of N–Dealkylation

QUATERNARY AMMONIUM SALTS

AMIDINES

GUANIDINES, ACYLGUANIDINES, AND BIGUANIDES

Acylguanidines

Biguanides

ANILINES

Metabolism

HYDRAZINES, ACYLHYDRAZINES, AND HYDRAZONES

ALDEHYDES

KETONES

CARBOXYLIC ACIDS

Metabolism

Bioisosteres of Carboxylic Acids

Amino Carboxylic Acids, N–Acyl Amino Acids, and Related Compounds

CARBOXYLIC ESTERS

AMIDES

LACTAMS AND IMIDES

Pyrazolone Antipyretics

Five–Membered Lactams as Nootropics

NITRILES

CARBONATES

CARBAMATES

Carbamates as Hypnotics

UREAS

THIOCARBONYL COMPOUNDS

SULFONIC ACIDS

SULFONIC ESTERS

SULFATES AND SULFAMIC ACIDS

PHOSPHONIC ACIDS

PHOSPHORIC ACID DERIVATIVES

N–(AMINOALKYL)BENZAMIDES, –BENZOATES, AND RELATED COMPOUNDS

ARYLALKYLAMINES

Antihistaminics: History

PHENETHYLAMINES (2–PHENYLETHYLAMINES)

Biological Activity of Phenethylamines

Metabolism

Tetrahydroisochinolines and Related Compounds

AMINOALKYLINDOLES AND INDOLE ALKALOIDS

PHENOTHIAZINES

Metabolism

DIBENZAZEPINES AND RELATED TRICYCLIC COMPOUNDS

3–ARYLOXY–2–HYDROXYPROPYLAMINES (B–ADRENERGIC ANTAGONISTS; ′B–BLOCKERS′)

Metabolism

OPIATES

N–(CARBOXYALKYL)–a–AMINO ACID AMIDES (PRILS)

ANILIDES AND AMIDES OF GLYCINE

PEPTIDES, PEPTIDOMIMETICS, AND RELATED OLIGOAMIDES

Peptidomimetics

Thrombin Inhibitors and Related Compounds

OLIGOARYLAMINES, OLIGOARYLAMIDES, OLIGOARYLCARBAMATES, AND OLIGOARYLUREAS

IMIDAZOLES

TRIAZOLES

PYRIDINES, PYRIMIDINES, AND RELATED COMPOUNDS

Proton Pump Inhibitors

QUINOLINES

Tecans

Quinazolines

NUCLEOSIDE ANALOGS

DIHYDROPYRIDINES

ARENESULFONAMIDES

Antibacterials

Diuretics

SULFONYLUREAS

BENZODIAZEPINES

STEROIDS

ANTHRACYCLINES

ARYLACETIC, BENZOIC, AND RELATED CARBOXYLIC ACIDS (NSAIDS)

Salicylates

QUINOLONECARBOXYLIC ACIDS (GYRASE INHIBITORS)

B–LACTAMS

Cephalosporins

PROSTAGLANDIN ANALOGS

SARTANS

STATINS

FOLIC ACID ANALOGS (ANTIFOLATES)

TAXANES

MACROCYCLIC COMPOUNDS
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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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