Project Details Analogue-based Drug Discovery II

Project No.:
Start Date:
01 June 2008
End Date:
01 July 2010
Division Name:
Chemistry and Human Health Division
Division No.:


The project under the title “Analogue-based Drug Discovery” has been successfully completed between 2003-2005 and the book, which has been published in 2006 by Wiley-VCH, was well received and all the copies have been sold in 18 months. Based on the positive feedbacks (see eg. M. Cowart, J. Med. Chem. 2006, 49, 4799) a continuation is needed.



The book consist of the following chapters:

Part I General Aspects
1 Optimizing Drug Therapy by Analogues
János Fischer, C. Robin Ganellin, John Proudfoot, and Erika M. Alapi

2 Standalone Drugs
János Fischer, C. Robin Ganellin, Arun Ganesan, and John Proudfoot

3 Application of Molecular Modeling in Analogue-Based Drug Discovery
György G. Ferenczy

4 Issues for the Patenting of Analogues
Stephen C. Smith

Part II Analogue Classes
5 Dipeptidyl Peptidase IV Inhibitors for the Treatment of Type 2 Diabetes
Jens-Uwe Peters and Patrizio Mattei

6 Phosphodiesterase 5 Inhibitors to Treat Erectile Dysfunction
Nils Griebenow, Helmut Haning, and Erwin Bischoff

7 Rifamycins, Antibacterial Antibiotics and Their New Applications
Enrico Selva and Giancarlo Lancini

8 Monoterpenoid Indole Alkaloids, CNS and Anticancer Drugs
András Nemes

9 Anthracyclines, Optimizing Anticancer Analogues
Federico-Maria Arcamone

10 Paclitaxel and Epothilone Analogues, Anticancer Drugs
Paul W. Erhardt and Mohammad El-Dakdouki

11 Selective Serotonin Reuptake Inhibitors for the Treatment of Depression
Wayne E. Childers Jr. and David P. Rotella

12 Muscarinic Receptor Antagonists in the Treatment of COPD
Matthias Grauert, Michael P. Pieper, and Paola Casarosa

13 b-Adrenoceptor Agonists and Asthma
Giovanni Gaviraghi

Part III Case Histories

14 Liraglutide, a GLP-1 Analogue to Treat Diabetes
Lotte B. Knudsen

15 Eplerenone: Selective Aldosterone Antagonist
Jaroslav Kalvoda and Marc de Gasparo

16 Clevudine, to Treat Hepatitis B Viral Infection
Ashoke Sharon, Ashok K. Jha, and Chung K. Chu

17 Rilpivirine, a Non-nucleoside Reverse Transcriptase Inhibitor to Treat HIV-1
Jerome Guillemont, Luc Geeraert, Jan Heeres, and Paul J. Lewi

18 Tipranavir, a Non-Peptidic Protease Inhibitor for Multi-drug Resistant HIV
Suvit Thaisrivongs, Joseph W. Strohbach, and Steve R. Turner

19 Lapatinib, an Anticancer Kinase Inhibitor
Karen Lackey

20 Dasatinib, a Kinase Inhibitor to Treat Chronic Myelogenous Leukemia
Jagabandhu Das and Joel C. Barrish

21 Venlafaxine and Desvenlafaxine, Selective Norepinephrine and Serotonin Reuptake Inhibitors to Treat Major Depressive Disorder
Magid Abou-Gharbia and Wayne E. Childers Jr.

The volume will discuss a broad spectrum of discoveries of anticancer, antifungal, antiviral, cardiovascular, CNS, diuretic, hormonal, respiratory, diabetes type 2 drugs.  The majority of the authors, who come from ten different countries, were also involved as inventor.


This project started in May 2008 and according to the chapters that are planned, 42 authors will participate.

> project announcement published in Chem. Int. Mar-Apr 2009

July 2010 – project completed – book published by Wiley-VCH, Weinheim, Analogue-based Drug Discovery II. 600 Pages, Hardcover, Handbook/Reference Book ISBN-10: 3-527-32549-2  ISBN-13: 978-3-527-32549-8; view content and sample chapter on WILEY ONLINE Library

The book is fetaured in Chem Int, Jul-Aug 2010, pp. 12-16

last update 20100723