Proceedings XIVth International Symposium on Medicinal Chemistry

Content: 
Advisory board
Page v

Preface
Page vii
Henk Timmerman

Some thoughts of the Editor
Page ix
Frans Awouters

The fungal cell wall as a drug discovery target: SAR of novel echinocandin analogs Original Research Article
Pages 1-13
James M. Balkovec, Regina M. Black, F. Aileen Bouffard, James F. Dropinski, Milton L. Hammond

Dual inhibition of angiotensin converting enzyme and neutral endopeptidase 24.11 Original Research Article
Pages 15-25
Shripad S. Bhagwat

Novel esterase-sensitive cyclic prodrugs of a model hexapeptide having enhanced membrane permeability and enzymatic stability Original Research Article
Pages 27-34
Sanjeev Gangwar, Giovanni M. Pauletti, Binghe Wang, Teruna J. Siahaan, Valentino J. Stella, Ronald T. Borchardt

Analogs of NPFF, a neuropeptide which modulates morphine analgesia Original Research Article
Pages 35-44
J.J. Bourguignon, V. Collot, B. Didier, J.P. Laulin, G. Simonnet

Chirality and kinetics Original Research Article
Pages 45-60
D.B. Campbell

Antidysrhythmic agents Original Research Article
Pages 61-70
S.F. Campbell

G proteins as drug targets Original Research Article
Pages 71-80
M. Freissmuth, M. Hohenegger, M. Waldhoer, S. Boehm, W. Beindl, C. Nanoff

Novel glycine antagonists as potent neuroprotective agents Original Research Article
Pages 81-95
Giovanni Gaviraghi, Romano Di Fabio, Alfredo Cugola, Daniele Donati, Aldo Feriani, Emiliangelo Ratti, David G. Trist, Angelo Reggiani

Hypertension — treatment by blockade of the Renin-Angiotensin system Original Research Article
Pages 97-107
W.J. Greenlee

Metabolism of endobiotics and therapeutic aspects of P450 inhibitors Original Research Article
Pages 109-116
R.W. Hartmann, M. Frotscher, G.L. Grün, M. Hector, D. Ledergerber, M. Mitrenga, T. Sergejew, G.A. Wächter

Cholesterol significantly affects drug interactions with membranes Original Research Article
Pages 117-125
Leo G. Herbette

Progress in the development of potent and selective cholinergic channel modulators (ChCMs) Original Research Article
Pages 127-136
Mark W. Holladay, Nan-Horng Lin, James P. Sullivan, Diana L. Donnelly-Roberts, Michael W. Decker, Jorge D. Brioni, James L. Ferrero, A. David Rodrigues, Kennan G. Marsh, Jerry G. Buccafusco, Stephen P. Arneric

Molecular modelling studies on histamine H2- and H3-receptor agonists Original Research Article
Pages 137-148
H.-D. Höltje, W. Sippl

aci-Reductones: Drug design, enantioselective syntheses and biological activities within lipid membranes Original Research Article
Pages 149-162
Allen T. Hopper, Andrei V. Blokhin, Venodhar K. Reddy, John Ziemniak, Donald T. Witiak

New methods for the preparation of optically pure nitrogen containing compounds of biological interest Original Research Article
Pages 163-173
Henri-Philippe Husson

Challenges and new directions in computer assisted structure based drug design Original Research Article
Pages 175-177
Peter Kollman

Biomimetic synthesis of racemic alkaloids Original Research Article
Pages 179-187
M.J. Wanner, G.J. Koomen

From monotherapy to multiple drug therapy through long-term pharmacology Original Research Article
Pages 189-203
Pierre M. Laduron

Challenges in antibacterial and antifungal drug discovery Original Research Article
Pages 205-218
Paul A. Lartey

Cytochrome P450 in the metabolism of xenobiotics and drug-drug interactions Original Research Article
Pages 219-230
G. Van\'t Klooster, K. Lavrijsen

Design and structure activity relationships of naphthalenic ligands of the melatonin receptors Original Research Article
Pages 231-239
D. Lesieur, V. Leclerc, I. Lesieur, P.J. Morgan, H.E. Howell, D.H. Caignard, P. Renard

From histamine H2 receptor regulation to a reclassification of H2 antagonists; inverse agonism as the basis for H2 receptor upregulation Original Research Article
Pages 241-250
Rob Leurs, Martine J. Smit, Astrid E. Alewijnse, Henk Timmerman

Interception of tyrosine kinase signaling pathways as a therapeutic modality Original Research Article
Pages 251-255
Alexander Levitzki

Chirality in drug design Original Research Article
Pages 257-269
D. Leysen

Dopamine D4 selective ligands as potential antipsychotics Original Research Article
Pages 271-290
J.-F. Liégeois, J. Bruhwyler

Combinatorial chemistry: a basic necessity inspired by nature\'s own approaches Original Research Article
Pages 291-306
R.M.J. Liskamp

Gene therapy for HIV-1 infection and AIDS Original Research Article
Pages 307-316
Julianna Lisziewicz

Signalling in the β-adrenergic receptor system Original Research Article
Pages 317-327
C. Krasel, M.J. Lohse

SAR and chemistry of glycopeptides active against multi-resistant bacteria Original Research Article
Pages 329-343
A. Malabarba, R. Ciabatti

In search of new peptides involved in cell-cell communication Original Research Article
Pages 345-354
Hisayuki Matsuo

Identification of the second extracellular loop in G-protein coupled neurotransmitter receptors as the site for ligand recognition, using spectral map analysis Original Research Article
Pages 355-370
Henri Moereels, Paul J. Lewi, Paul A.J. Janssen

Structure-based design of epitope mimetics Original Research Article
Pages 371-381
E.E. Moret, R.M.J. Liskamp, J.P. Tollenaere

Functional characterization of novel G protein-coupled receptors involved in nociception and HIV-1 infection Original Research Article
Pages 383-396
M. Samson, C. Mollereau, J. Rucker, F. Libert, B.J. Doranz, C. Liesnard, Y. Yi, R.J. Smyth, F. Liners, R.G. Collman, J. Costentin, J.-C. Meunier, R. Doms, G. Vassart, M. Parmentier

Structure-activity relationships in a series of C2-symmetric HIV-protease inhibitors Original Research Article
Pages 397-408
A. Peyman, K.-H. Budt, B. Stowasser, J. Hansen, L. Jian-Qi, J. Knolle, C. Meichsner, A. Paessens, D. Ruppert, J. Spanig, I. Winkler

Medicinal chemistry as we start the next millennium Original Research Article
Pages 409-419
Philip S. Portoghese

Constitutively active α1B-adrenergic receptor mutants: Potential mechanisms underlying receptor activation Original Research Article
Pages 421-431
A. Scheer, F. Fanelli, T. Costa, P.G. de Benedetti, S. Cotecchia

CI-1011: An atypical ACAT inhibitor with antiatherosclerotic activity Original Research Article
Pages 433-441
D.R. Sliskovic

Angiogenesis and (anti)angiogenic drugs Original Research Article
Pages 443-450
H.A.J. Struijker Boudier, F.A.C. le Noble

Anti-atherosclerotics - Bile acid sequestrants, cholesterol absorption and fibrates Original Research Article
Pages 451-459
K.E. Suckling

Cardiovascular new drug discovery of the future: Molecules, genes, and machines Original Research Article
Pages 461-476
Pieter B.M.W.M. Timmermans, Ronald D. Smith

The action of serpins and heparin as leads in drug discovery Original Research Article
Pages 477-486
C.A.A. van Boeckel, P. Westerduin, J. Basten, C.M. Dreef-Tromp, D.G. Meuleman, R.G.M. van Amsterdam, P.D.J. Grootenhuis

Inverse isostere strategies in the development of cholinergic agonists with multiple therapeutic potentials Original Research Article
Pages 487-498
J.S. Ward, L. Merritt, D.O. Calligaro, F.P. Bymaster, H.E. Shannon, C.H. Mitch, M.J. Sheardown, P.H. Olesen, M.D.B. Swedberg, P. Sauerberg

Computer-aided design of novel inhibitors of human leukocyte elastase Original Research Article
Pages 499-509
D. Andisik, P. Bernstein, F. Brown, C. Bryant, C. Ceccarelli, J. Damewood, P. Edwards, S. Feeney, B. Gomes, R. Green, B. Kosmider, A. Shaw, G. Steelman, R. Thomas, P. Tuthill, E. Vacek, C. Veale, P. Warner, J. Williams, D. Wolanin,  et al.

Antiplatelet agents Original Research Article
Pages 511-535
Ruth R. Wexler

ucbL059, A new antiepileptic agent with a novel mode of action Original Research Article
Pages 537-553
E. Wülfert

Index of authors
Pages 555-557

Subject index
Pages 559-561