The goal of an activity-directed isolation process is to isolate bioactive compounds which may provide structural leads of therapeutic importance. Whereas the traditional process of drug development is long and expensive, simple and rapid bioassays can serve as the starting point for drug discovery. This book presents a range of "bench top" bioassay techniques useful for natural product and pharmaceutical chemists involved in drug discovery and pharmacognosy. The contents detail a number of enzyme-based assays, cell-based functional bioassays and receptor radioligand binding assays along with detailed descriptions of each type. The majority of these bioassays are presented in a step-by-step format, so they could even be implemented by technical personnel with little background in microbiology, biochemistry or pharmacology.

The spectacular advances of medicinal chemistry in the last few decades have been triggered by a greater understanding of cellular processes at the molecular level. The understanding of biochemical processes and diseases at molecular level has revolutionized the field. This volume summarizes recent developments in the area of biological inhibitors such as squalene epoxidase inhibitors, dual inhibitors of 5-lipoxygenase and cycloxgenase, inhibition of cholestrol biosynthesis, HIV proteinase inhibitors, nonpeptide antagonists at peptide receptors, and binding interaction of thyroid hormones.