Archived: 1st Winter Conference
on Medicinal & Bioorganic Chemistry
January 29th - February 2nd 1995
Steamboat Springs Resort, Colorado
Agenda
Sunday, January 29th 1995
Monsanto/NSERC Symposium on Stereoselective Synthesis in Medicinal Chemistry
Program Chair: Dr Victor Snieckus, University of Waterloo
Overview: Recent Methods in Peptidomimetic Assemblage
Peptide Secondary Structure Mimetics: Recent Advances and Future Challenges
Peptidomimetics in Drug Design: Orakky Bioavailable Inhibitors of HIV Protease
Asymetric Syntheses: Highly Enantioselective Carbon-carbon Bond Formations Vased on Asymmetric Deprotonation of Carbamate Esters
Enantio- and Diastereoselective Syntheses of Aminoalcohols and Related Compounds via Asymmetric Deprotonation of Carbamate Esters
The Total Syntheses of Rapamycin and Dimethoxyrapamycin
Applications of Stereoselective Synthesis in Bioorganic Chemistry
New Stereocontrolled Methods for Ring Formation
Recent Advances in the Synthesis of Bioactive Natural Products
Monday, January 30th 1995
Molecular Mechanism of Signal Transduction
Program Chair: Dr Grant Krafft, Northwestern University Medical Center
Cellular Modes of Signal Transduction: An Overview
Integration of Signal Transduction Pathways Regulated By Heterotrimeric G-Proteins and Tyrosine Kinases
Signalling via TNFα Receptor
G-Proteins in Signal Transduction
SH2 Domains and Inhibitors
Nuclear Signal Transduction
Steroid Superfamily Receptors: Prototypic Ligand-Gated Transcription Factors
Tuesday, January 31st 1995
KEYNOTE | “Molecular Probes for Steroid Receptors: Structure, Modeling and Medical Imaging”
Program Chair: Prof. John A. Katzenellenbogen, University of Illinois
General Oral Papers | Session I
Program Chair: Mike Rafferty
Tirilizad Mesylate: A Novel and Effective Treatment for Acute Neurologic Disorders, Mechanism of Action and Pharmacology
Rational Design of Non-peptide Renin Inhibitors
Structure-Based Inhibitors of Influenza Viral Neuraminidase. Development of a Benzoic Acid Lead
Bioreversible Analogs of Oligonucleotides: Stereospecific Conversion of S-alkyl Phosphorothiolates to Phosphorothioates
Amino Acid Phosphoramidates of Antiviral Nucleosides Exhibit High Potency and Low Toxicity
Discovery of a Novel Pos-Translational Isomerization of Ser46 in ω-Aga-IVB and ω-Aga-IVC, Calcium Channel Toxins Isolated from the Agelenopsis Aperta Spider
Photoaffinity Probes of DNA Polymerase Structure and Function
Rigid Analogs of Camptothecin as DNA Topoisomerase Inhibitors
General Oral Papers | Session II
Program Chair: Dan Flynn
Linker Design for β-Turn Formation
Stereo-Control in the Convergent Synthesis of Chiral Carbocyclic Nucleoside Analogues
Synthetic Approaches to Taxol and Analogs
Structure-Based Drug Design and Optimization of HIV Protease Inhibitors
Microsphere Formation and Drug Delivery in a Series of Derivatized Amino Acids
Synthesis and Evaluation of Pyridyl Analogs of L-735,524: Potent HIV Protease Inhibitors
Wortmannin Analogs are Potent Inhibitors of Photsphatidylinositol-3-Kinase
Novel 1,2-Diarylcyclopentenes are Potent, Selective, and Orally Active COX-2 Inhibitors
Evening Poster Program
Conformationally Restricted, Nonpeptide Fibrinogen Receptor Antagonists: Design and Synthesis of Orally Active, Long Acting Inhibitors of GPIIB/IIIA Mediated Platelet Aggregation
Enantioslective Synthesis of the Dual 5-HT4/5-HT3 Serotonergic Agent SC-52491
Aminodiol Inhibitors of HIV Protease: Modifications at P2 which Enhance Potency
A Conformationally Defined 6-S-trans-Retinoic Acid Isomer with Chemoprotective Activity and Toxicity Comparable to Retinoic Acid
Predicting the Activites of Taxol Analogues Using CoMFA
Photochemical Cycloaromatization Reactions of ortho-Dialkynylarenes. New DNA Photocleaving Agents
Synthesis and Characterization of Fruan Dihydrofuran Analogs of the Dopamine D3 Ligand 7-OH-DPAT
Synthesis and Biological Activities of Balanol Analogs as Protein Kinase C Inhibitors: A Study of Carboxylic Acid Replacementts
Synthesis of 13-epi- Taxol via Transannular Delivery of a Borohydride Reagent
Synthesis of [35S] 3H-1,2- BEnzodithiole-3-one-1,1- Dioxide: Application in the Preparation of Site-specifically 35S-Labeled Oligonucleotides
High Affinity Partial Agonist Imidazo [1,5-a]quinoxaline Piperazine Ureas at the GABAa/Benzodiazepine Receptor Complex
The Design, Synthesis, and Pharmacology of the Potent, Orally Active LTB4 Antagonist, CP-105696
Design and Synthesis of Phosphorus and Hydroxamate Inhibitors of Endothelin Converting Enzyme
Photoprobes of Nucleic Acid Polymerase Substrate Blinding Sites
The Rational Design and Synthesis of Potent, Nonpeptide Endothelin Receptor Antagonists
Selective Manipulation of the Pampamycin Effector Domain: Synthesis and Evaluation of C-7 Derivatives and the X-ray Crystal Structures of their Complexes with FKBP12
Preparation and Evaluation of Substituted 1,4,7,8,9,10-Hexahydropyrido [4,3-fjquinoxaline-2,3-diones as AMPA Receptor Antagonists
Classical Hansch Analysis and Comparative Molecular Field Analysis (CoMFA) of the Phenylethanolamine N-Methyltransferase (PNMT) Inhibitory Activity of Benzylamines
Stereoselective Synthesis of Novel Methylene Ether Dipeptide Isosteres
Spatially Diverse Libraries for Pharmaceutical Lead Discovery
2-Aryl Substituted Dipyridodiazeoinones are Potent Inhibitors of HIV-1 Reverse Transcriptase and Possess Activity Against the Y181C Mutant Enzyme
Synthesis and Binding Affinity of 2,3,3a,4,9,9a-Hexahydro-(Iminomethano)-1H-Benz[f]indenes. Ligands for the PCP site of the NMDA Receptor.
Cycloalkylpyranones: A New Template for the Design of Potent, Non-Peptidic HIV Protease Inhibitors
Carboline and Carbazole Derivatives of K252C as Potential Small Molecule Neurotrophic Agents
Novel Antipsychotics with Unique D2/5-HT1a Affinity and Minimal Extrapyramisal Side-Effect Liability
An Improved Method for Synthesizing C24,C25-Substituted Avermectins
Equilibrium in Bromomethylation of 5-Cyclopropyl-3-Hydroxyisoxazole
A Novel Assymetric Synthesis of Atropisomeric 6-Aryl Pyrazinores via an Unusual Chirality Transfer Process
Toward the Total Synthesis of (-)-Sparteine
Novel Substituted Pipecolinic Amide Dertivatives as HIV Protease Inhibitors
Molecular Modelling of the Phenylpiperidine Antagonist LY-255582 with Other Opioids Suggests a Model of Antagonist and Agonist Binding to Opioid Receptors
Wednesday, February 1st 1995
Recent Advances in Enzyme Inhibitor Discovery
Program Chair: Dr Daniel Rich, University of Wisconsin
Overview: Recent Advances in Enzyme Inhibitor Discovery
Novel Enzyme Kinetic Mechanisms
Application of Combinatorial Chemistry to the Determination of Novel Inhibitors for Proteases
Structure-based Design of HIV Protease Inhibitors
Thrombin and Factor Xa Inhibitors
Rational Design of HIV Protease Inhibitors
HIV Protease Inhibitors: Nonpeptide Leads from Compound Collections
Novel HIV Protease Inhibitor Templates
Thursday, February 2nd 1995
The Re-emergence of Natural Products as a Source of New Therapeutics
Program Chair: Dr Lester Mitscher, University of Kansas
Introduction, Historical Considerations, and Overview
Higher Plants with Anticancer and Antifungal Activity
Higher Plants with Antiviral and Other Activities