*** 9761164 West This Small Business Innovation Research Phase I project is directed at developing a new technology for generating bio-active libraries of compounds for high-throughput screening in drug discovery. This new synthesis method is expected to create a diverse spectrum of large numbers of drug candidate compounds - many with structures that are difficult or impossible to obtain with other methods. The Phase I program will produce eight libraries of compounds, where each library is created from reactants with structural similarities to ligands for targeted receptors. The libraries generated will be screened for binding to cannabinoid and x-opioid receptors. Phase I success will be established if binding is demonstrated at a rate of at least one in 1000 screened compounds - an order of magnitude improvement over current 'hit rates" achieved by combinatorial chemistry techniques. The proposed process has great commercial potential as a tool for the discovery of new drugs. With the advent of high-throughput screening techniques, there is a great demand in the pharmaceutical industry for new compounds. If successful, this new process will produce large numbers of an extremely diverse range of compounds. ***