Drug Design : Medicinal Chemistry: A Series of Monographs, Vol. 5

Drug Design, Volume V covers the fundamental approaches to the development of bioactive compounds. The book discusses the utilization of operational schemes for analog synthesis in drug design; the design of enzyme inhibitors (transition state analogs); and the significance of structure-absorption-distribution relationships for drug design. The text describes the role of charge-transfer processes in the action of bioactive materials, as well as the approaches to the rational combination of antimetabolites for cancer chemotherapy. The physicochemical, quantum chemical, and other theoretical techniques for the understanding of the mechanism of action of central nervous system (CNS) agents, such as psychoactive drugs, narcotics, and narcotic antagonists and anesthetics, are also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable. Content: MEDICINAL CHEMISTRY: A Series of Monographs , Page ii Front Matter , Page iii Copyright , Page iv List of Contributors , Pages ix-x Preface , Page xi , E.J. ARIËNS Contents of Other Volumes , Pages xiii-xvii Chapter 1 - Diphenhydramine Derivatives: Through Manipulation toward Design , Pages 1-80 , A.F. Harms, W. Hespe, W.Th. Nauta, R.F. Rekker, H. Timmerman, J. de Vries Chapter 2 - The Design of Antiradiation Agents , Pages 81-142 , Daniel L. Klayman, Edmund S. Copeland Chapter 3 - Rational Approach to Proteinase Inhibitors , Pages 143-169 , Shosuke Okamoto, Akiko Hijikata Chapter 4 - The Design of Organ-Imaging Radiopharmaceuticals , Pages 171-259 , Raymond E. Counsell, Rodney D. Ice Chapter 5 - Design of X-Ray Contrast Media , Pages 261-295 , Hans-Joachim Herms, Volker Taenzer Chapter 6 - Agricultural Pesticides: Chemical and Physical Methods of Formulation , Pages 297-351 , G.S. Hartley Subject Index , Pages 353-364 Drug Design, Volume VI covers practical approaches to the development of bioactive compounds, with focus on antiradiation agents, organ-imaging radiopharmaceuticals, X-ray contrast media, proteinase inhibitors, and pesticide formulations. The book discusses the chemical routes available for the synthesis of diphenhydramine derivatives, the biological activities, the relationships between structure and activity, and the phase of manipulation in the design of diphenhydramine derivatives. The text also describes the design of antiradiation agents, organ-imaging radiopharmaceuticals, and X-ray contrast media, as well as the rational approach to proteinase inhibitors. The chemical and physical methods of formulation of agricultural pesticides are also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design and manufacture will find the book invaluable.