Born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together ...
Born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together constitute the first systematic approach to drug analog development.
Of interest to virtually every researcher working in drug discovery and pharmaceutical chemistry.
"Analogue-Based Drug Discovery II is a companion book to the first volume ... This volume provides an excellent overview of several biological targets, compound classes, and illustrations of problem solving in medicinal chemistry for chemists in drug discovery who are beginning to establish their careers" (ChemMedChem, 1 January 2012)
Janos Fischer is a Senior Research Scientist at Richter Plc., Budapest, Hungary. He received his MSc and PhD degrees in organic chemistry from the Eotvos University of Budapest under Professor A. Kucsman. Between 1976 and 1978, he was a Humboldt Fellow at the University of Bonn under Professor W. Steglich. He has worked at Richter Plc. since 1981 where he participated in the research and development of leading cardiovascular drugs in Hungary. His main interest is analogue based drug discovery. He is the author of some 100 patents and scientific publications. In 2004, he was elected as a Titular member of the Chemistry and Human Health Division of IUPAC. He received an honorary professorship at the Technical University of Budapest.
C. Robin Ganellin studied Chemistry at London University, receiving a PhD in 1958 under Professor Michael Dewar, and was a Research Associate at MIT with Arthur Cope in 1960. He then joined Smith Kline & French Laboratories in the UK and was one of the co inventors of the revolutionary drug, cimetidine (also known as Tagamet). In 1986, he was made a Fellow of the Royal Society and appointed to the SK&F Chair of Medicinal Chemistry at University College London, where he is now Professor Emeritus of Medicinal Chemistry. Professor Ganellin is co inventor of over 160 patents and has authored over 260 scientific publications. He was President of the Medicinal Chemistry Section of the IUPAC and is Chairman of the IUPAC Subcommittee on Medicinal Chemistry and Drug Development.
PART I GENERAL ASPECTS
Optimizing Drug Therapy by Analogues
Application of Molecular Modeling in Analogue-Based Drug Discovery
Issues for the Patenting of Analogues
PART II ANALOGUE CLASSES
Dipeptidyl Peptidase IV Inhibitors for the Treatment of Type 2 Diabetes
Phosphodiesterase 5 Inhibitors to Treat Erectile Dysfunction
Rifamycins, Antibacterial Antibiotics and Their New Applications
Monoterpenoid Indole Alkaloids, CNS Anticancer Drugs
Anthracyclines, Optimizing Anticancer Analogues
Paclitaxel and Epothilone Analogues, Anticancer Drugs
Selective Serotonin Reuptake Inhibitors for the Treatment of Depression
Muscarinic Receptor Antagonists in the Treatment of COPD
beta-Adrenoceptor Agonists and Asthma
PART III CASE HISTORIES
Liraglutide, a GLP-1 Analogue to Treat Diabetes
Eplerenone: Selective Aldosterone Antagonist
Clevudine, to Treat Hepatitis B Viral Infection
Rilpivirine, a Non-nucleoside Reverse Transcriptase Inhibitor to Treat HIV-1
Tipranavir, a Non-Peptidic Protease Inhibitor for Multi-drug Resistant HIV
Lapatinib, an Anticancer Kinase Inhibitor
Dasatinib, a Kinase Inhibitor to Treat Chronic Myelogenous Leukemia
Venlafaxine and Desvenlafaxine, Selective Norepinephrine and Serotonin Reuptake Inhibitors to Treat Major Depressive Disorder