XIVth International Symposium on Medicinal ChemistryBy
- F. Awouters, Janssen Research Foundation, Turnhoutse Weg 30, 2340 Beerse, Belgium
Vaso-occlusive disorders including unstable angina, myocardial infarction, transient ischemic attacks, stroke and peripheral artery disease remain the major sources of morbidity and mortality in western civilization. Platelet activation and resulting platelet aggregation play a major role in the pathogenesis of these thromboembolic diseases. Recognition of the contribution of platelets to the pathophysiology of cardiovascular disease has provided impetus for the continued search for new antiplatelet agents. Hence, over the past two decades many strategies have been evaluated in the search for efficacious mechanisms to reduce platelet function. The medical need for more efficacious antithrombotic drugs and the growing understanding of the role of platelets in vascular injury have catalyzed the extensive evaluation of novel approaches to control platelet function. Along these lines, the volume therefore provides an in-depth assessment of ongoing clinical trials, new and clinically established agents, and other developments in this rapidly developing field.
Published: September 1997
- Introduction. 1. The fungal cell wall as a drug discovery target: SAR of novel echinocandin analogs. 2. Dual inhibition of angiotensin converting enzyme and neutral endopeptidase. 3. Novel esterase-sensitive cyclic prodrugs of a model hexapeptide having enhanced membrane permeability and enzymatic stability. 4. Analogs of NPFF a neuropeptide which modulate morphine analgesia. 5. Chirality and Kinetics. 6. Antidyrhythmic agents. 7. G proteins and drug targets. 8. Novel glycine antagonists as potent neuroprotective agents. 9. Hypertension-treatment by blockade of the renin-angiotensin system. 10. Metabolism of endobiotics and therapeutic aspects of P450 inhibitors. 11. Cholesterol significantly affects drug interactions with membranes. 12. Progress in the development of potent and selective cholinergic channel modulators (ChCMs). 13. Molecular modelling studies on histamine H2- and H3-receptor agonists. 14. aci-Reductones: Drug design, enantioselective syntheses and biological activities within lipid membranes. 15. New methods for the preparation of optically pure nitrogen containing compounds of biological interest. 16. Challenges and new directions in computer assisted structure based drug design. 17. Biomimetic synthesis of racemic alkaloids. 18. From monotherapy to multiple drug therapy through long term pharmacology. 19. Challenges in antibacterial antifungal drug discovery. 20. Cytochrome P450 in the metabolism of xenobiotics and drug-drug interactions. 21. Design and structure activity relationships of naphthalenic ligands of the melatonin receptors. 22. From histamine H2 receptor regulation to a reclassification of H2 antagonists: inverse agonisms as the basis for H2 receptor upregulation. 23. Interception of tyrosine kinase signaling pathways as a therapeutic modality. 24. Chirality in drug design. 25. Dopamine D4 selective ligands as potential antipsychotics. 26. Combinatorial chemistry: a basic necessity inspired by nature's own approaches. 27. Gene therapy for HIV-1 infection and aids. 28. Signalling in the &bgr;-adrenergic receptor system. 29. SAR and chemistry of glycopeptides active against multi-resistant bacteria. 30. In search of new peptides involved in cell-cell communication. 31. Identification of the second extracellular loop in G-protein neurotransmitter receptors as a site for ligand recognition, using spectral map analysis. 32. Structure-based design of epitope mimetics. 33. Functional characterization of novel G.protein-coupled receptors involved in nociception and HIV-1 infection. 34. Structure-activity relationships in a series of C2-symmetric HIV-protease inhibitors. 35. Medicinal chemistry as we start the next millennium. 35. Constitutively active &agr; 1 B-adrenergic receptor mutants: potential mechanisms underlying receptor activation. 37. Cl-1011: an atypical ACAT inhibitor with antiatherosclerotic activity. 38. Angiogenesis and (anti)angiogenic drugs. 39. Anti-atherosclerotics -bile acid sequrstrants, cholesterol absorption and fibrates. 40. Cardiovascular new drug discovery of the future: molecules, genes and machines. 41. The action of serpins and heparin as leads in drug discovery. 42. Inverse isostere strategies in the developments of coleinergic agonists with multiple therapeutic potentials. 43. Computer-aided design of novel inhibitors of human leukocyte elastase. 44. Antiplatelet agents. 45. ucb L059, a new antiepileptic agent with a novel mode of action. Index of authors. Subject index.