Preface. Insights into the structure and function of genetic disease genes from genome research and clues for drug therapy (P.L. Pearson). Structure-based design: fact or fiction? (P.D.J. Grootenhuis et al.). New developments in synthetic medicinal chemistry (F. Gualtieri) . New biocatalytic approaches for the synthesis of chiral drugs, intermediates, and substrates (K. Laumen et al.). ∝ -Diazorcarbonyl chemistry- target driven applications (R. Pellicciari et al.) Ligands for the 5-HT 2C receptor as potential antidepressents and anxiolytics (D.Leysen, J. Kelder). 5-HT 1A-affinity, activity and selectivity versus D2-receptors of flesinoxan and analogues N-Arylpiperazines (W. Kuipers). Serotonin transmission in depression and anxiety disorders - new insights and potential new drugs (M. Briley, C. Moret). Pharmacokinetics and metabolism in drug development: current and future strategies (D.D. Breimer). Novel approaches towards anti-HIV chemotherapy (E. de Clercq). PMEA and PMPA: acyclic nucleoside phosphonates with potent anti-HIV activity (T. Cihlar, N. Bischofberger). HBY 097 - a second-generation nonnucleoside inhibitor of the HIV-1 reverse transcriptase (J-P. Kleim). The HIV tat-TAR interaction, a novel target for drug discovery (J. Karn et al.). Diverse approaches to combinatorial library design (E.J. Martin et al.). Heterocyclic mixture- based combinatorial libraries: synthesis and analysis of composition (J.S. Kiely, Y. Pei). The quest of new chemical entities to treat the gastric pathogen Helicobacter pylori (T.C. Kühler). Chemistry and SAR of prokinetic motilides: non peptidic motilin receptor agonists (P.A. Lartey). Modulators of 5-HT functions in the treatment of gastrointestinal disorders (F.D. King et al.). The impact of robotics and novel assay technologies on lead discovery processes (J.G. Houston). New animal models in target discovery (R.S. Oosting et al.). Hot topics (P. Angeli). Inverse agonism at G protein-coupled receptors. Studies with wild type and mutated adrenergic and opioid receptors (G. Milligan). Life and death decisions: medicinal chemistry approaches to apoptosis (A.P. Kozikowski). Antibiotic resistance - a view from the pharmaceutical industry (R. Bax).
This volume of Pharmacochemistry Library comprises the text of invited lectures presented at the 11th Noordwijkerhout-Camerino Symposium Trends in Drug Research, held in Noordwijkerhout, The Netherlands, from 11-15 May 1997.
In the programme attention has been given to the generation of new biological target systems and the generation of new lead molecules, with presentations on e.g. combinatorial chemistry, compound libraries, database search, high throughput screening and molecular biology.
Other topics discussed were the perspectives for new medicines for the gastro-intestinal tract, the major developments in the search for effective anti-HIV drugs and new aspects in synthetic approaches. In a special session three topics which currently draw much attention were discussed: How to deal with the major problem of resistance against antimirobial agents? Can the apoptosis mechanism be used as a drug target? Is the newly observed phenomenon of inverse agonism a general principle and has it consequences for drug development (and use?)
Clinical pharmacologists, pharmaceutics and toxicologists
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- © Elsevier Science 1998
- 16th January 1998
- Elsevier Science
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Vakgroep Farmacochemie, Vrije Universiteit Amsterdam, De Boele Laan 1083, 1081 HV Amsterdam, The Netherlands