Medicinal Chemistry : A Series of Monographs, Vol. 11. Drug Design: Parts 1-10

Contents: Vol. I. Preface. 1. A general introduction to the field of drug design/E.J. Ariens. 2. Quantitative structure--activity relationships in drug design/Corwin Hansch. 3. Physicochemical approaches to the rational development of new drugs/J.K. Seydel. 4. A molecular orbital approach to quantitative drug design/A.J. Wohl. 5. Electronic aspects of drug action/Roger L. Schnaare. 6. The role of biopharmaceutics in the design of drug products/John G. Wagner. 7. Significance of pharmacokinetics for drug design and the planning of dosage regimens/J.M. van Rossum. Author index. Subject index.

Vol. II. Preface. 1.    Modulation of pharmacokinetics by molecular manipulation/E.J. Ariens. 2. Factors in the design of reversible and irreversible enzyme inhibitors/Howard J. Schaeffer. 3. The design of organophosphate and carbamate inhibitors of cholinesterases/R.D. O\'Brien. 4. The design of reactivators for irreversibly blocked acetylcholinesterase/I.B. Wilson and Harry C. Froede. 5. Inhibition of protein biosynthesis: its significance in drug design/Arthur P. Grollman. 6. Enzymes and their synthesis as a target for antibiotic action/M.H. Richmond. 7. The rational design of antiviral agents/Arthur P. Grollman and Susan B. Horwitz. 8. Design of penicillins/A.E. Bird and J.H.C. Nayler. 9. The design of peptide hormone analogs/J. Rudinger. 10. Recent advances in the design of diuretics/George de Stevens. 11. Design of biologically active steroids/G.A. Overbeek, J. van der Vies and J. de Visser. 12. Rational elements in the development of superior neuromuscular blocking agents/M. Martin-Smith. 13. The design of tumor-inhibitory alkylating drugs/J.A. Stock. Author index. Subject index.

Vol. III. Preface. 1. Microbial conversion as a tool in the preparation of drugs/R. Beukers, A.F. Marx and M.H.J. Zuldweg. 2. The use of linear free energy parameters and other experimental constants in structure--activity studies/A. Verloop. 3. Anticoagulants structurally and functionally related to vitamin K/T. Kralt and V. Claassen. 4. Design of B-blocking drugs/A.M. Barrett. 5. The design of biologically active acridines/Adrien Albert. 6. The design of local anesthetics/J. Buchi and X. Perlia. 7. Design of insect chemosterilants/Ralph B. Turner. 8. Molecular approach for designing inhibitors to enzymes involved in blood clotting/L. Lorand and J.L.G. Nilsson. Author index. Subject index.

Vol. IV. Preface. 1. Biopharmaceutics as a basis for the design of drug products/Leslie Z. Benet. 2. Peroral solid dosage forms with prolonged action/W.A. Ritschel. 3. Parenteral dosage forms with prolonged action/W.A. Ritschel. 4. Design of topical drug products: pharmaceutics/Martin Katz. 5. Design of topical drug products: biopharmaceutics/Boyd J. Poulsen. 6. The design of sunscreen preparations/Goswin W. van Ham and Wolfgang P. Herzog. 7. Litholytic agents: preventive and curative drugs for nephrolithiasis/George Kallistratos. 8. The design of biologically active nucleosides/Alexander Bloch. 9. The design of insecticidal chlorohydrocarbon derivatives/G.T. Brooks. Author index. Subject index.

Vol. V. Preface. 1. Utilization of operational schemes for analog synthesis in drug design/John G. Topliss and Yvonne C. Martin. 2. The design of enzyme inhibitors: transition state analogs/R.N. Lindquist. 3. Structure-absorption-distribution relationships: significance for drug design/Eric J. Lien. 4. The role of charge-transfer processes in the action of bioactive materials/Peter H. Doukas. 5. Approaches to the rational combination of antimetabolites for cancer chemotherapy/Gerald B. Grindey, Richard G. Moran and William G. Werkheiser. 6. Physicochemical, quantum chemical and other theoretical techniques for the understanding of the mechanism of action of CNS agents: psychoactive drugs, narcotics, and narcotic antagonists and anesthetics/Joyce J. Kaufman and Walter S. Koski. Subject index.

Vol. VI. Preface. 1. Diphenhydramine derivatives: through manipulation toward design/A.F. Harms, W. Hespe, W. Th. Nauta, R.F. Rekker, H. Timmerman and J. de Vries. 2. The design of antiradiation agents/Daniel L. Klayman and Edmund S. Copeland. 3. Rational approach to proteinase inhibitors/Shosuke Okamoto and Akiko Hijikata. 4. The design of organ-imaging radiopharmaceuticals/Raymond E. Counsell and Rodney D. Ice. 5. Design of x-ray contrast media/Hans-Joachim Herms and Volker Taenzer. 6. Agricultural pesticides: chemical and physical methods of formulation/G.S. Hartley. Subject index.

Vol. VII. Preface. 1. The design of artificial blood substitutes/Robert P. Geyer. 2. Insect pheromones as a basis for the development of more effective selective pest control agents/F.J. Ritter and C.J. Persoons. 3. The design of auxin-type herbicides/J.L. Garraway and R.L. Wain. 4. Development and application of new steric substituent parameters in drug design/A. Verloop, W. Hoogenstraaten and J. Tipker. 5. Computer technology in drug design/Paul J. Lewi. Index.

Vol. VIII. Preface. 1. Advances in the methodology of quantitative drug design/Yvonne C. Martin. 2. The application of pattern recognition to drug design/Gerald L. Kirschner and Bruce R. Kowalski. 3. The design of controlled drug delivery systems/S.K. Chandrasekaran, F. Theeuwes and S.I. Yum. 4. Receptor binding as a tool in the development of new bioactive steroids/J.P. Raynaud, T. Ojasoo, M.M. Bouton and D. Philibert. 5. The design of synthetic sweeteners/Guy A. Crosby, Grant E. DuBois and Robert E. Wingard, Jr. 6. The prospective assessment of environmental effects of chemicals/E.H. Hueck-van der Plas and H.J. Hueck. 7. Design of selective ion binding macrocyclic compounds and their biological applications/Reed M. Izatt, John D. Lamb, Delbert J. Eatough, James J. Christensen and J. Howard Rytting. Index.

Vol. IX. Preface. 1. Design of safer chemicals/E.J. Ariens. 2. Consequences of the Hansch paradigm for the pharmaceutical industry/Stefan H. Unger. 3. A physical chemical basis for the design of orally active prodrugs/Samuel H. Yalkowsky and Walter Morozowich. 4. The masca model of pharmacochemistry: I. Multivariate statistics/Peter P. Mager. 5. Rationales in the design of rectal and vaginal delivery forms of drugs/C.J. de Blaey and J. Polderman. 6. Interactive graphics in medicinal chemistry/Edgar F. Meyer, Jr. 7. Logico-structural approach to computer-assisted drug design/V.E. Golender and A.B. Rozenblit. Index.

Vol. X. Preface. 1. Practical procedures in drug design/V. Austel and E. Kutter. 2. Structural aspects of the structure--activity relationships of neuroleptics: principles and methods/J.P. Tollenaere, H. Moereels and L.A. Raymaekers. 3. Bridging the gap between bioactive peptides and nonpeptides: some perspectives in design/P.S. Farmer. 4. Dynamic systems analysis as a basis for drug design: application to antihypertensive drug action/H.A.J. Struyker-Boudier. 5. Polymeric drug delivery systems/Sung Wan Kim, Robert V. Petersen and Jan Feijen. 6. The design of biocompatible polymers/T. Gilchrist and J.M. Courtney. 7. The design of insect repellents/W.A. Skinner and H.L. Johnson. 8. Multivariate data analysis in structure--activity relationships/Paul J. Lewi. 9. The masca model of pharmacochemistry: II. Rational empiricisms in the multivariate analysis of opioids/Peter P. Mager. Index.

From the preface of Part X: "The positive responses to the previous volumes of Drug Design and the rapid development in this field have encouraged and stimulated us to continue this series.

The first two chapters examine procedures as a applied in the practice of drug design. Chapter 3, "Bridging the gap between bioactive peptides and nonpeptides," opens promising perspectives in the highly actual field of bioactive peptides. A new physiological approach to drug design, i.e. "Dynamic systems analysis as a basis for drug design," is outlined in chapter 4, and chapters 5 and 6 deal effectively with polymers in drug design in "Polymeric drug delivery systems" and "The design of biocompatible polymers," respectively. Chapter 7 presents the structure--activity relationships of insect repellents as a basis for the design of such agents, and chapters 8 and 9 give approaches to the multivariate data analysis in structure--activity relationships, which is an essential aspect of drug design.

Again, as in previous volumes, the aim of the authors has been to offer the reader insights into promising and current developments in the field. The topics are presented in an informative, concise, systematic, and thought-provoking manner, in which speculations and new perspectives are encouraged. The contents of this volume and those preceding it are indicative of the wide scope, the interdisciplinary character, and the various perspectives of drug design, a discipline in which fundamental and applied science go hand in hand."