Plenary Lectures Presented At The Third International Symposium On Bioorganic Chemistry Held In Dagomys Russia 17 23 September 1995

Volume 4 of Advances in Medicinal Chemistry is comprised of six chapters on a wide range of topics in medicinal chemistry, including molecular modeling, structure-based drug design, organic synthesis, peptide conformational analysis, biological assessment, structure-activity correlation, and lead optimization. Chapter 1 presents an account about amino acid-based peptide mimetics corresponding to b-turn, loop, helical motifs in proteins as a probe of ligand-receptor and ligand-enzyme molecular interactions. Chapter 2 addresses new facets of the medicinal chemistry of the important anticancer drug Taxol® (paclitaxel). Chapter 3 relates an account of the search for new drugs for the treatment of malaria based on the natural product artemisinin. Chapter 4 applies computational chemistry to the evaluation of compound libraries for biological testing. Chapter 5 describes the construction of a 3-dimensional molecular model of the human thrombin receptor, the first protease-activated G-protein coupled receptor (PAR-1), as a means to explore the intermolecular contacts involved in agonist peptide recognition. Finally, Chapter 6 describes the research conducted at Merck on inhibitors of farnesyl transferase as a potential treatment for human cancers.

Carbohydrate chemistry provides access to carbohydrate-based natural products and synthetic molecules as useful biologically active structures relevant to many health care and disease-related biological processes. Recent Trends in Carbohydrate Chemistry: Synthesis, Structure, and Function of Carbohydrates covers green and sustainable reactions, organometallic carbohydrate chemistry, synthesis of glycomimetics, multicomponent reactions, and chemical transformations leading to molecular diversity based on carbohydrates. These include inhibitors of glycogen phosphorylase, which are relevant in controlling type 2 diabetes and sugar sulfates. Polysaccharides, which are commonly modified chemically, are also examined with contributions covering polysaccharide synthesis and modification of polysaccharides to obtain new structures and properties. Recent Trends in Carbohydrate Chemistry: Synthesis, Structure, and Function of Carbohydrates is ideal for researchers working as synthetic organic chemists, and for those interested in biomolecular chemistry, green chemistry, organometallic chemistry, and material chemistry in academia as well as in industry Demonstrates the importance of carbohydrate chemistry as green and sustainable chemistry Details monosaccharide syntheses and transformations toward biologically active small molecular entities Provides the most recent findings on polysaccharide synthesis and bioapplications