Advances in Medicinal Chemistry: Volume 4

Klappentext 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. Inhaltsverzeichnis Preface. Novel peptide mimetic building blocks and strategies for efficient lead finding. Recent advances in the medicinal chemistry of taxoid anticancer agents. Synthesis and structure-activity relationships of peroxidic antimalarials based on artemisinin. Design of compound libraries for detecting and pursuing novel small molecule leads. A theoretical model of the human thrombin receptor (PAR-1), the first known protease-activated G-protein-coupled receptor. Farnesyl transferase inhibitors: design of a new class of cancer chemotherapeutic agents.

Zusammenfassung
Comprises of six chapters on a 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.

Inhalt

Preface. Novel peptide mimetic building blocks and strategies for efficient lead finding. Recent advances in the medicinal chemistry of taxoid anticancer agents. Synthesis and structure-activity relationships of peroxidic antimalarials based on artemisinin. Design of compound libraries for detecting and pursuing novel small molecule leads. A theoretical model of the human thrombin receptor (PAR-1), the first known protease-activated G-protein-coupled receptor. Farnesyl transferase inhibitors: design of a new class of cancer chemotherapeutic agents.