Lead Optimization for Medicinal Chemists

Pharmacokinetic Properties of Functional Groups and Organic Compounds

Inbunden, Engelska, 2012

Av Florencio Zaragoza Dörwald, Switzerland) Zaragoza Dorwald, Florencio (Lonza AG, Visp

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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.

Produktinformation

Utgivningsdatum2012-04-18
Mått178 x 246 x 33 mm
Vikt1 325 g
FormatInbunden
SpråkEngelska
Antal sidor622
FörlagWiley-VCH Verlag GmbH
ISBN9783527332267

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Florencio Zaragoza Dorwald studied chemistry at the Georg-August University in Gottingen, Germany, and Universite 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.

PART I: Introduction THE DRUG DISCOVERY PROCESSPharmacokinetics -Structure RelationshipThe Future of Small-Molecule Drugs LEAD OPTIMIZATIONWhat 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 ALKANESMetabolism ALKENES AND ALKYNESMetabolism ARENESMetabolism HALIDESFluorineChlorineBromineIodineAlkylating Agents AZIDES NITRO COMPOUNDSMetabolism AZO COMPOUNDS TRIAZENES NITRATES AND NITRITES N-NITROSO COMPOUNDS N-OXIDES ALCOHOLSMetabolism PHENOLS ETHERSMetabolism EPOXIDES PEROXIDES THIOLS THIOETHERSMetabolism SULFOXIDES SULFONES ALIPHATIC AMINESBasicityMetabolismRates of N-Dealkylation QUATERNARY AMMONIUM SALTS AMIDINES GUANIDINES, ACYLGUANIDINES, AND BIGUANIDES AcylguanidinesBiguanides ANILINESMetabolism HYDRAZINES, ACYLHYDRAZINES, AND HYDRAZONES ALDEHYDES KETONES CARBOXYLIC ACIDSMetabolismBioisosteres of Carboxylic AcidsAmino Carboxylic Acids, N-Acyl Amino Acids, and Related Compounds CARBOXYLIC ESTERS AMIDES LACTAMS AND IMIDESPyrazolone AntipyreticsFive-Membered Lactams as Nootropics NITRILES CARBONATES CARBAMATESCarbamates as Hypnotics UREAS THIOCARBONYL COMPOUNDSSULFONIC ACIDS SULFONIC ESTERS SULFATES AND SULFAMIC ACIDS PHOSPHONIC ACIDS PHOSPHORIC ACID DERIVATIVES N-(AMINOALKYL)BENZAMIDES, -BENZOATES, AND RELATED COMPOUNDS ARYLALKYLAMINESAntihistaminics: History PHENETHYLAMINES (2-PHENYLETHYLAMINES)Biological Activity of PhenethylaminesMetabolismTetrahydroisochinolines and Related Compounds AMINOALKYLINDOLES AND INDOLE ALKALOIDS PHENOTHIAZINESMetabolism 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 OLIGOAMIDESPeptidomimeticsThrombin Inhibitors and Related Compounds OLIGOARYLAMINES, OLIGOARYLAMIDES, OLIGOARYLCARBAMATES, AND OLIGOARYLUREAS IMIDAZOLES TRIAZOLES PYRIDINES, PYRIMIDINES, AND RELATED COMPOUNDSProton Pump Inhibitors QUINOLINESTecansQuinazolines NUCLEOSIDE ANALOGS DIHYDROPYRIDINES ARENESULFONAMIDESAntibacterialsDiuretics SULFONYLUREAS BENZODIAZEPINES STEROIDS ANTHRACYCLINES ARYLACETIC, BENZOIC, AND RELATED CARBOXYLIC ACIDS (NSAIDS)Salicylates QUINOLONECARBOXYLIC ACIDS (GYRASE INHIBITORS) B-LACTAMSCephalosporins PROSTAGLANDIN ANALOGS SARTANS STATINS FOLIC ACID ANALOGS (ANTIFOLATES) TAXANES MACROCYCLIC COMPOUNDS