Trends in Drug Research II, Proceedings of the 11th Noordwijkerhout-Camerino Symposium

Henk van der Goot (Eds.)0444826335, 9780444826336

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?)

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Table of contents :
Content:
Preface
Page VII
H. Timmerman

Insights into the structure and function of genetic disease genes from genomeresearch and clues for drug therapy Original Research Article
Pages 1-6
P.L. Pearson

Structure-based design: fact or fiction? Original Research Article
Pages 7-14
P.D.J. Grootenhuis, R.M.A. Knegtel, J.C. Heikoop, C.A.A. van Boeckel

New developments in synthetic medicinal chemistry Introduction Original Research Article
Pages 15-16
F. Guatieri

New biocatalytic approaches for the synthesis of chiraldrugs, intermediates, and substrates Original Research Article
Pages 17-28
Kurt Laumen, André Brunella, Martin Graf, Matthias Kittelmann, Paula Walser, Oreste Ghisalba

α-Diazocarbonyl chemistry—Target driven applications Original Research Article
Pages 29-47
R. Pellicciari, G. Costantino, M. Marinozzi, L. Mattoli, B. Natalini

Ligands for the 5-HT2C receptor as potential antidepressants and anxiolytics Original Research Article
Pages 49-61
D. Leysen, J. Kelder

5-HT1A-affinity, activity and selectivity versus D2-receptors of flesinoxan andanalogous N-arylpiperazines Original Research Article
Pages 63-74
Wilma Kuipers

Serotonin transmission in depression and anxiety disorders—new insightsand potential new drugs Original Research Article
Pages 75-84
M. Briley, C. Moret

Pharmacokinetics and metabolism in drug development: current and future strategies Original Research Article
Pages 85-89
D.D. Breimer

Novel approaches towards anti-HIV chemotherapy Original Research Article
Pages 91-104
Erik De Clercq

PMEA and PMPA: Acyclic nucleoside phosphonates with potent anti-HIV activity Original Research Article
Pages 105-116
T. Cihlar, N. Bischofberger

HBY 097—a second-generation nonnucleoside inhibitor of the HIV-1 reverse transcriptase Original Research Article
Pages 117-119
Jörg-Peter Kleim

The HIV tat-TAR interaction, a novel target for drug discovery Original Research Article
Pages 121-132
Jonathan Karn, Nicholas J. Keen, Mark J. Churcher, Fareed Aboul-ela, Gabriele Varani, François Hamy, Eduard R. Felder, Gerhard Heizmann, Thomas Klimkait

Diverse approaches to combinatorial library design Original Research Article
Pages 133-146
Eric J. Martin, Roger E. Critchlow, David C. Spellmeyer, Steven Rosenberg, Kerry L. Spear, Jeffrey M. Blaney

Heterocyclic mixture-based combinatorial libraries:synthesis and analysis of composition Original Research Article
Pages 147-156
J.S. Kiely, Y. Pei

The quest for new chemical entities to treat the gastric pathogen Helicobacter pylori Original Research Article
Pages 157-165
Thomas C. Kühler

Chemistry and SAR of prokinetic motilides: non-peptidic motilin receptor agonists Original Research Article
Pages 167-178
P.A. Lartey

Modulators of 5-HT functions in the treatment of gastrointestinal disorders Original Research Article
Pages 179-190
F.D. King, L.M. Gaster, G.J. Sanger, K.A. Wardle

The impact of robotics and novel assay technologies on lead discovery processes Original Research Article
Pages 191-202
John G. Houston

New animal models in target discovery Original Research Article
Pages 203-213
R.S. Oosting, K.L. Stark, R. Hen, G.J.M. van Scharrenburg

Hot topics Original Research Article
Pages 215-217
P. Angeli

Inverse agonism at G protein-coupled receptors. Studies with wild type and mutated adrenergic and opioid receptors Original Research Article
Pages 219-224
G. Milligan

Life and Death decisions: Medicinal chemistry approaches to apoptosis Original Research Article
Pages 225-235
Alan P. Kozikowski

Antibiotic resistance — a view from the pharmaceutical industry Original Research Article
Pages 237-241
R. Bax

Author index
Page 243

Subject index
Pages 245-247