Antiparasitic and antibacterial drug discovery : from molecular targets to drug candidates

Mainly addressing parasitic diseases but also focusing on diseases caused by bacteria, this much-needed reference and handbook provides a unique insight into the approach adopted by commercial science towards infectious diseases, including the work of medicinal chemists. Many of the authors are scientists with hands-on experience of drug discovery units within the pharmaceutical industry. In addition, the text covers efforts towards drug development in infectious diseases from academic groups and non profit organizations.Content: Chapter 1 Target Identification and Mechanism?Based Screening for Anthelmintics: Application of Veterinary Antiparasitic Research Programs to Search for New Antiparasitic Drugs for Human Indications (pages 1–15): Timothy G. Geary, Debra J. Woods, Tracey Williams and Solomon NwakaChapter 2 Anthelmintic Resistance as a Guide to the Discovery of New Drugs? (pages 17–32): Georg v. Samson?Himmelstjerna, Roger K. Prichard and Adrian J. WolstenholmeChapter 3 Drug Discovery for Neglected Diseases: View of A Public–Private Partnership (pages 33–43): Rob Don and Eric ChatelainChapter 4 Bioinformatics and Chemoinformatics: Key Technologies in the Drug Discovery Process (pages 45–57): Andreas Krasky, Andreas Rohwer, Richard J. Marhofer and Prof. Dr. Paul M. SelzerChapter 5 Target Identification and Validation in Antiparasitic Drug Discovery (pages 59–73): Christian Wolf and Nikolas GunkelChapter 6 Selective Drug Targets in Parasites (pages 75–98): Peter Kohler and Richard J. MarhoferChapter 7 Lessons Learned from Target?Based Lead Discovery (pages 99–115): Michael Gassel, Jorg Cramer, Christopher Kern, Sandra Noack and Wolfgang StreberChapter 8 Approaches towards Antiparasitic Drug Candidates for Veterinary Use (pages 117–133): Christophe Chassaing and Harald SekljicChapter 9 Learning to Relate Structural Space to Property Space (pages 135–158): Michael Berger, Jorg Cramer, Michael Hinz, Christina Mertens, Christian Miculka, Trevor Newton, Jorg Schroder and Harald SekljicChapter 10 Recruiting the Host Defense Mechanisms: Roles for Vaccines and Chemotherapeutics (pages 159–173): Theo P. M. SchettersChapter 11 Proteases of Parasitic Protozoa – Current Status and Validation (pages 175–209): Mohammed Sajid, Michael J. Blackman, Patricia Doyle, Chen He, Kirkwood M. Land, Cheryl Lobo, Zachary Mackey, Momar Ndao, Sharon L. Reed, Brian Shiels, Ryan Swenerton and William WeirChapter 12 In Search of Trypanocidal Drugs (pages 211–226): Leopold FloheChapter 13 Trypanosomatid Protein Kinases as Potential Drug Targets (pages 227–247): Martin Wiese, Andrew Morris and Karen M. GrantChapter 14 Targeting the Malaria Kinome: Discovering Kinase Inhibitors as Novel Antimalarial Agents (pages 249–276): Dayadevi Jirage, Susan M. Keenan and Norman C. WatersChapter 15 Malaria and Antimalarials – A Focused View (pages 277–298): Frank SeeberChapter 16 Chemotherapeutic Development Strategies for Schistosomiasis (pages 299–321): Conor R. Caffrey, David L. Williams, Matthew H. Todd, David L. Nelson, Jennifer Keiser and Jurg UtzingerChapter 17 Searching New Antiparasitics in Virtual Space (pages 323–338): Frank Oellien, Kristin Engels, Jorg Cramer, Richard J. Marhofer, Christopher Kern and Prof. Dr. Paul M. SelzerChapter 18 Cyclooctadepsipeptides – An Anthelmintically Active Class of Compounds Exhibiting a Novel Mode of Action (pages 339–356): Achim Harder, Kathryn Bull, Marcus Guest, Lindy Holden?Dye and Robert WalkerChapter 19 Chemical Optimization of Anthelmintic Compounds – A Case Study (pages 357–371): Thorsten Meyer, Jorg Schroder, Manfred Uphoff, Sandra Noack, Anja R. Heckeroth, Michael Gassel, Petra Rohrwild and Thomas IlgChapter 20 Pathogenomics: Identification of Novel Drug Targets and Vaccine Candidates in Bacteria (pages 373–413): Knut Ohlsen, Martin Eckart, Ulrich Dobrindt, Heike Bruhn and Jorg HackerChapter 21 Tuberculosis Drug Discovery: Issues, Gaps and the Way Forward (pages 415–440): Veronique Dartois, Franz Joel Leong and Thomas DickChapter 22 Decreasing the Number of Gaps in the Draft Assembly of the Mannheimia Haemolytica M7/2 Genome Sequence (pages 441–451): Hon Q. Tran, Mathias Beig, Volker Spehr, Andreas Rohwer, Gottfried Unden and Prof. Dr. Paul M. SelzerChapter 23 Total Synthesis and Configurational Assignment of Pasteurestin A and B, a Natural Product with Antimicrobial Activity on Pasteurellaceae (pages 453–471): Marion Kogl, Lothar Brecker, Ralf Warrass and Johann Mulzer Content: Preamble Editor Preface PART I Drug Discovery Approaches 1 Target identification and mechanism-based screening for anthelmintics: Application of veterinary antiparasitic research programmes to search for new antiparasitic drugs for human indications 2 Anthelmintic resistance as a guide to the discovery of new drugs? 3 Drug discovery for neglected diseases: view of a public-private partnership 4 Bioinformatics and Chemoinformatics: Key Technologies in the Drug Discovery Process 5 Target identification and validation in anti parasitic drug discovery 6 Selective Drug Targets in Parasites 7 Lessons Learned From Target Based Lead Discovery 8 Approaches towards Antiparasitic Drug Candidates for Veterinary Use 9 Learning to Relate Structural Space with Property Space 10 Recruiting the Host Defense Mechanisms: Roles for Vaccines and Chemotherapeutics PART II Protozoan Parasites 11 Proteases of Parasitic Protozoa - Current Status and Validation 12 In Search of Trypanocidal Drugs 13 Trypanosomatid protein kinases as potential drug targets 14 Targeting the malaria kinome discovering kinase inhibitors as novel antimalarial agents 15 Malaria and anti-malarials - a focused view PART III Multicellular Parasites 16 Chemotherapeutic development strategies for schistosomiasis 17 Searching new Anti-Parasitics in the Virtual Space 18 Cyclooctadepsipeptides - an anthelmintically active class of compounds exhibiting a novel mode of action 19 Chemical Optimization of Anthelmintic Compounds - a Case Study PART IV Bacteria 20 Pathogenomics: identification of novel drug targets and vaccine candidates in bacteria 21 Tuberculosis Drug Discovery: Issues, Gaps and the Way Forward 22 Decreasing the number of gaps in the draft assembly of the Mannheimia haemolytica M7/2 genome sequence 23 Total synthesis and configurational assignment of pasteurestin A and B, a natural product with antimicrobial acitivty on Pasteurellaceae " ... An interesting book that leads the reader through what factors can influence drug discovery and then gives specific examples on the current situation in development of drugs for particular parasitic and bacterial diseases."--ChemMedChem, 2009Addressing parasitic diseases and those caused by bacteria, this much needed reference and handbook provides a unique insight into the approach adopted by commercial science towards infectious diseases, including the work of medicinal chemists. Many of the authors are scientists with hands-on experience of drug discovery units within the pharmaceutical Addressing parasitic diseases and those caused by bacteria, this much-needed reference and handbook provides a unique insight into the approach adopted by commercial science towards infectious diseases, including the work of medicinal chemists. Many of the authors are scientists with hands-on experience of drug discovery units within the pharmaceutical industry. In addition, the text covers efforts towards drug development in infectious diseases from academic groups and non profit organizations Addressing parasitic diseases and diseases caused by bacteria, this much-needed reference and handbook provides a unique insight into the approach adopted by academic and commercial science towards infectious diseases, including the work of medicinal chem