Edited by Eric M. Gordon and James F. Kerwin, Jr.
Increasing pressure to identify, optimize, develop, and commercialize novel drugs more rapidly and more cost–effectively has led to an urgent demand for technologies that can reduce the time to market for new products. Molecular diversity, of both natural and synthetic materials, provides a valuable source of compounds for identifying and optimizing new drug leads. Through the rapidly evolving technology of combinatorial chemistry, it is now possible to produce libraries of small molecules to screen for novel bioactivities. This powerful new technology has begun to help pharmaceutical companies find new drug candidates quickly, save significant dollars in preclinical development costs, and ultimately change their fundamental approach to drug discovery.
Comprising the work of the leading authorities in the area of molecular diversity and combinatorial chemistry, Combinatorial Chemistry and Molecular Diversity in Drug Discovery highlights the critical concepts and issues involved in implementing combinatorial chemistry to create chemical libraries. The authors, industrial and academic experts in the field, apply combinatorial technologies to drug discovery and development and place co–evolving technologies and practices in a global framework.
Included among the many topics:
∗ Historical background.
∗ Library strategy and design.
∗ Solid–phase synthesis.
∗ Small molecular libraries.
∗ Automation, analytical, and computational methodology.
∗ Biological diversity.
∗ Strategies for screening combinatorial libraries.
∗ Combinatorial drug screening and development.
∗ Combinatorial chemistry information management.
Combinatorial Chemistry and Molecular Diversity in Drug Discovery is one of the first comprehensive books to cover this explosive area. It is must reading for medicinal chemists, pharmacologists, molecular biologists, biochemists, enzymologists, and drug discovery research managers in industry, academia, and government.
COMBINATORIAL CHEMISTRY AND MOLECULAR DIVERSITY: AN INTRODUCTION.
Historical Overview of the Developing Field of Molecular Diversity (J. Chabala, et al.).
Solid–Phase Peptide Synthesis, Lead Generation, and Optimization (B. Seligman, et al.).
Oligonucleotide Libraries as a Source of Molecular Diversity (H.–Y. Mei, et al.).
SMALL MOLECULAR LIBRARIES.
Protease Inhibitor Libraries (D. Patel & D. Campbell).
Scaffolds for Small Molecule Libraries (M. Pavia).
Encoded Combinatorial Chemistry (J. Jacobs & Z.–J. Ni).
Parallel Organic Synthesis in Array Format (S. Hall).
AUTOMATION, ANALYTICAL, AND COMPUTATIONAL METHODS.
Automation of Combinatorial Chemistry for Large Libraries (M. Needels & J. Sugarman).
Quantifying Diversity (Y. Martin, et al.).
Protein Scaffolds for Peptide Libraries (R. Hoess).
Strategies for Screening Combinatorial Libraries (B. Beutel).
COMBINATORIAL DRUG SCREENING AND DEVELOPMENT.
Combinatorial Technologies: Prospects and Future Issues (J. Kerwin).