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Molecular Diversity and Combinatorial Chemistry : Libraries and Drug Discovery - I.M. Chaiken

Molecular Diversity and Combinatorial Chemistry

Libraries and Drug Discovery

By: I.M. Chaiken (Editor), K.D. Janda (Editor)

Hardcover Published: 19th March 2001
ISBN: 9780841234505
Number Of Pages: 340

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Reports progress on chemical, enzymatic, phage, and cell-derived libra ries. Discusses synergy between structure-based design and combinatori al libraries. Presents applications of combinatorial libraries to drug discovery and new synthetic catalysis. Reports library screening appr oaches, including the use of NMR. Presents recent advances in solid-ph ase organic synthesis, liquid-phase organic synthesis, and high-throug hput combinatorial organic synthesis. Discusses automation of organic synthesis as well as new methodologies for monitoring solid-phase orga nic synthesis.

Prefacep. ix
Secondary Structure Templated Libraries: Mimicking Naturep. 2
Construct Diversity: A New Paradigm for Combinatorial Chemistryp. 10
Enhancing the Drug Discovery Process by Integration of High-Throughput Chemistry and Structure-Based Drug Designp. 16
Library Design: Solid-, Solution-, and Liquid-Phase Combinatorial Synthesis
Phosphorus as a Scaffold: Combinatorial Libraries of Non-nucleotide Phosphoramidatesp. 30
Convergent Solid-Phase Synthesis of Phosphoramidate Combinatorial Librariesp. 40
Solid-Phase Synthesis, Characterization, and Screening of a 43,000-Compound Tetrahydroisoquinoline Combinatorial Libraryp. 50
Solid-Phase and Combinatorial Synthesis of Heterocyclic Scaffolds: Dihydropyridines, Pyridines, and Pyrido [2,3-d] pyrimidinesp. 58
Polymer-Supported Chemistry: Synthesis of Small-Ring Heterocyclesp. 70
A Solution-Phase Strategy for the Parallel Synthesis of Chemical Libraries Containing Small Organic Molecules: A General Dipeptide Mimetic and a Flexible General Templatep. 81
Structurally Homogeneous and Heterogeneous Libraries: Scaffold-Based Libraries and Libraries Built Using Bifunctional Building Blocksp. 99
Liquid-Phase Combinatorial Synthesisp. 118
Libraries of Transition-Metal Catalysts: High-Throughput Screening of Catalysts for Synthetic Organic Methodologyp. 128
Mixtures of Molecules Versus Mixtures of Pure Compounds on Polymeric Beadsp. 137
Biology-Based Chemical Libraries
Generation of Solution-Phase Libraries of Organic Molecules by Combinatorial Biocatalysisp. 144
Living Libraries Using Gene Transfer: A Renaissance for Natural Productsp. 158
Phage Expression of a De Novo Designed Coiled Coil Stem Loop Miniprotein Scaffold for Constrained Peptide Library Displayp. 172
Automated Solid-Phase Synthesis
Automation of High-Throughput Synthesis: Automated Laboratory Workstations Designed To Perform and Support Combinatorial Chemistryp. 188
Boosting the Productivity of Medicinal Chemistry Through Automation Tools: Novel Technological Developments Enable a Wide Range of Automated Synthetic Proceduresp. 199
A Modular System for Combinatorial and Automated Synthesisp. 207
LiBrain: Software for Automated Design of Exploratory and Targeted Combinatorial Librariesp. 219
Automation Issues at the Interface Between Combinatorial Chemistry and High-Throughput Screeningp. 233
Analytical Methods and Screening
Tools for Combinatorial Chemistryp. 246
Magic-Angle Spinning NMR Spectroscopy of Polystyrene-Bound Organic Molecules: MOnitoring a Three-Step Solid-Phase Synthesis Involving a Heck Reactionp. 255
A High-Throughput Functional Assay for G-Protein-Coupled Receptors: Method for Screening Combinatorial Librariesp. 273
Use of Combinatorial Libraries in the Discovery and Development of Novel Anti-infectivesp. 284
Application of Polymer-Supported Chemistry to the Discovery and Optimization of Lead Drug Candidatesp. 298
Using Pharmacophore Diversity To Select Molecules To Test from Commercial Cataloguesp. 309
Author Indexp. 317
Affiliation Indexp. 318
Subject Indexp. 318
Table of Contents provided by Syndetics. All Rights Reserved.

ISBN: 9780841234505
ISBN-10: 0841234507
Series: Conference Proceeding Series
Audience: General
Format: Hardcover
Language: English
Number Of Pages: 340
Published: 19th March 2001
Publisher: American Chemical Society
Country of Publication: US
Dimensions (cm): 23.77 x 15.8  x 2.72
Weight (kg): 0.68