Successful drug discovery. Volume 1 / edited by János Fischer and David P. Rotella.

Format:

Book

Contributor:

Fischer, János, editor.

Rotella, David P., editor.

Language:

English

Subjects (All):

Drugs--Design.

Drugs.

Pharmaceutical chemistry.

Physical Description:

1 online resource (578 p.)

Edition:

1st ed.

Place of Publication:

Weinheim, [Germany] : Wiley-VCH Verlag, 2015.

Language Note:

English

Summary:

The first volume of the book series ""Successful Drug Discovery"" isfocusing on new drug discoveries during the last decade, fromestablished drugs to recently introduced drugs of all kinds:small-molecule-, peptide-, and protein-based drugs.The role of serendipity is analyzed in some very successful drugswhere the research targets of the lead molecule and the drug aredifferent. Phenotypic and target-based drug discovery approachesare discussed from the viewpoint of pioneer drugs and analogues.This volume gives an excellent overview of insulin analoguesincluding a discussion of the properties of

Contents:

Cover; Related Titles; Title Page; Copyright; Advisory Board Members; Preface; Part I: General Aspects; Part II: Drug Class; Part III: Case Histories; Chapter 1: Serendipitous Target-Based Drug Discoveries; 1.1 Introduction; 1.2 Recent Examples of Target-Based Drug Discovery; 1.3 Serendipitous Target-Based Drug Discoveries; 1.4 Drospirenone (Contraceptive with Anti-aldosterone Activity); 1.5 Escitalopram (Selective Serotonin Reuptake Inhibitor Antidepressant); 1.6 Ezetimibe (Inhibitor of Cholesterol Absorption); 1.7 Lamotrigine (Discovery of a Standalone Drug for the Treatment of Epilepsy)

1.8 Omeprazole (Proton Pump Inhibitor Acid-Suppressive Agent)1.9 Outlook; Acknowledgments; List of Abbreviations; References; Chapter 2: Drug Discoveries and Molecular Mechanism of Action; 2.1 Introduction; 2.2 Mechanistic Paradox; 2.3 Molecular Mechanism of Action; 2.4 How MMOAs were Discovered; 2.5 Case Study: Artemisinin; 2.6 Summary; List of Abbreviations; References; Chapter 3: Insulin Analogs - Improving the Therapy of Diabetes; 3.1 Introduction; 3.2 Pharmacology and Insulin Analogs; 3.3 Chemical Description; 3.4 Rapid-Acting Insulin Analogs (Prandial or Bolus Insulin)

3.5 Long-Acting Insulin Analog Formulations (Basal Insulin)3.6 Conclusions and Future Considerations; List of Abbreviations; References; Chapter 4: The Discovery of StendraTM (Avanafil) for the Treatment of Erectile Dysfunction; 4.1 Introduction; 4.2 Discovery of Avanafil; 4.3 Pharmacological Features of Avanafil; 4.4 Clinical Studies of Avanafil; 4.5 Conclusion; List of Abbreviations; References; Chapter 5: Dapagliflozin, A Selective SGLT2 Inhibitor for Treatment of Diabetes; 5.1 Introduction; 5.2 Role of SGLT2 Transporters in Renal Function; 5.3 O-Glucoside SGLT2 Inhibitors

5.4 m-Diarylmethane C-Glucosides5.5 Profiling Studies with Dapagliflozin; 5.6 Clinical Studies with Dapagliflozin; 5.7 Summary; List of Abbreviations; References; Chapter 6: Elvitegravir, A New HIV-1 Integrase Inhibitor for Antiretroviral Therapy; 6.1 Introduction; 6.2 Discovery of Elvitegravir; 6.3 Conclusion; List of Abbreviations; References; Chapter 7: Discovery of Linagliptin for the Treatment of Type 2 Diabetes Mellitus; 7.1 Introduction; 7.2 Discovery of Linagliptin - High Throughput Screening Hit Optimization

7.3 Rationalization of DPP-4 Inhibition Potency by Crystal Structure Analysis and Studies of Binding Kinetics7.4 Basic Physicochemical, Pharmacological, and Kinetic Characteristics; 7.5 Preclinical Studies; 7.6 Clinical Studies; 7.7 Conclusion; List of Abbreviations; References; Chapter 8: The Discovery of Alimta (Pemetrexed); List of Abbreviations; References; Chapter 9: Perampanel: A Novel, Noncompetitive AMPA Receptor Antagonist for the Treatment of Epilepsy; 9.1 Introduction; 9.2 Seeds Identification by High Throughput Screening (HTS) Assays

9.3 Structure and Activity Relationship (SAR) Study Starting from the Unique Structure of Seed Compounds

Notes:

Description based upon print version of record.

Includes bibliographical references and index.

Description based on online resource; title from PDF title page (ebrary, viewed March 23, 2015).

ISBN:

9783527678457

352767845X

9783527678433

3527678433

9783527678440

3527678441

OCLC:

902846601