Topics in Medicinal Chemistry

Part 1 Neuropeptides: multiple receptors for substance P and related tachykinins; design of novel antagonists of cholecystokynin; novel approaches to the pharmacological modification of peptidergic neurotransmission; pharmacological consequences of conformational restriction in opioid peptides; "peptoids" from CCK-8. Part 2 Control of enzymatic processes in medicinal chemistry: enzyme inhibition - approaches to drug design; studies on renin inhibitors; rational design of enzyme inhibitors containing small rings; amino-sugar derivatives and related compounds as glycosidase inhibitors. Part 3 Antiviral agents: the mechanism of action and selectivity of the antiherpetic drug acyclovir; synthesis of some antiviral carbocyclic nucleosides; the development of agents active against herpes viruses and human immunodeficiency virus; new purine derivatives with selective antiviral activity. Part 4 Antibacterial, antifungal and antiparasitic agents: recent developments in avermectin research; fluconazole - a novel systemically active antifungal agent; antimalarial hydroxynaphthoquinones; approaches to the synthesis of antibacterial compounds. Part 5 Applications of computing to medicinal chemistry: a rational approach to the design of antihypertensives - X-Ray studies of complexes between aspartic proteinases and aminoalcohol renin inhibitors; computing and trial and error in chemotherapeutic research; application of molecular dynamics in the prediction of accessible conformations.