Awouters XIVth International Symposium on Medicinal Chemistry

1. Auflage 1997
ISBN: 978-0-08-054388-8
Verlag: Elsevier Science & Techn.
Format: PDF
Kopierschutz: 1 - PDF Watermark

E-Book, Englisch, 560 Seiten, Web PDF

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.

Autoren/Hrsg.

Awouters, F.

Inhaltsverzeichnis

1;Front Cover;1
2;Pharmacochemistry Library, Volume 28;4
3;Copyright Page;5
4;Contents;12
5;Preface;8
6;Some thoughts of the Editor;10
7;Chapter 1. The fungal cell wall as a drug discovery target: SAR of novel echinocandin analogs;16
8;Chapter 2. Dual inhibition of angiotensin converting enzyme and neutral endopeptidase 24.11;30
9;Chapter 3. Novel esterase-sensitive cyclic prodrugs of a model hexapeptide having enhanced membrane permeability and enzymatic stability;42
10;Chapter 4. Analogs of NPFF a neuropeptide which modulate morphine analgesia;50
11;Chapter 5. Chirality and Kinetics;60
12;Chapter 6. Antidyrhythmic agents;76
13;Chapter 7. G proteins and drug targets;86
14;Chapter 8. Novel glycine antagonists as potent neuroprotective agents;96
15;Chapter 9. Hypertension-treatment by blockade of the renin-angiotensin system;112
16;Chapter 10. Metabolism of endobiotics and therapeutic aspects of P450 inhibitors;124
17;Chapter 11. Cholesterol significantly affects drug interactions with membranes;132
18;Chapter 12. Progress in the development of potent and selective cholinergic channel modulators (ChCMs);142
19;Chapter 13. Molecular modelling studies on histamine H2- and H3-receptor agonists;152
20;Chapter 14. aci-Reductones: Drug design, enantioselective syntheses and biological activities within lipid membranes;164
21;Chapter 15. New methods for the preparation of optically pure nitrogen containing compounds of biological interest;178
22;Chapter 16. Challenges and new directions in computer assisted structure based drug design;190
23;Chapter 17. Biomimetic synthesis of racemic alkaloids;194
24;Chapter 18. From monotherapy to multiple drug therapy through long term pharmacology;204
25;Chapter 19. Challenges in antibacterial antifungal drug discovery;220
26;Chapter 20. Cytochrome P450 in the metabolism of xenobiotics and drug-drug interactions;234
27;Chapter 21. Design and structure activity relationships of naphthalenic ligands of the melatonin receptors;246
28;Chapter 22. From histamine H2 receptor regulation to a reclassification of H2 antagonists: inverse agonisms as the basis for H2 receptor upregulation;256
29;Chapter 23. Interception of tyrosine kinase signaling pathways as a therapeutic modality;266
30;Chapter 24. Chirality in drug design;272
31;Chapter 25. Dopamine D4 selective ligands as potential antipsychotics;286
32;Chapter 26. Combinatorial chemistry: a basic necessity inspired by nature's own approaches;306
33;Chapter 27. Gene therapy for HIV-1 infection and aids;322
34;Chapter 28. Signalling in the ß-andrenergic receptor system;332
35;Chapter 29. SAR and chemistry of glycopeptides active against multi-resistant bacteria;344
36;Chapter 30. In search of new peptides involved in cell-cell communication;360
37;Chapter 31. Identification of the second extracellular loop in G-protein neurotransmitter receptors as a site for ligand recognition, using spectral map analysis;370
38;Chapter 32. Structure-based design of epitope mimetics;386
39;Chapter 33. Functional characterization of novel G protein-coupled receptors involved in nociception and HIV-1 infection;398
40;Chapter 34. Structure-activity relationships in a series of C2-symmetric hiv-protease inhibitors;412
41;Chapter 35. Medicinal chemistry as we start the next millennium;424
42;Chapter 36. Constitutively active a1B-adrenergic receptor mutants: potential mechanisms underlying receptor activation;436
43;Chapter 37. CI-1011: An atypical ACAT inhibitor with antiatherosclerotic activity;448
44;Chapter 38. Angiogenesis and (anti)angiogenic drugs;458
45;Chapter 39. Anti-Atherosclerotics - bile acid sequestrants, cholesterol absorption and fibrates.;466
46;Chapter 40. Cardiovascular new drug discovery of the future: molecules, genes, and machines;476
47;Chapter 41. The action of serpins and heparin as leads in drug discovery;492
48;Chapter 42. Inverse isostere strategies in the development of cholinergic agonists with multiple therapeutic potentials;502
49;Chapter 43. Computer-aided design of novel inhibitors of human leukocyte elastase;514
50;Chapter 44. Antiplatelet agents;526
51;Chapter 45. ucb L059, a new antiepileptic agent with a novel mode of action.;552
52;Index of authors;570
53;Subject index;574