E. J. Ariens – författare

Physico-Chemical Aspects of Drug Action, Volume 7 covers topics on drug kinetics and the overall physicochemical properties of the drug in relation therewith, and the physicochemical aspects of the drug-receptor interaction, putting emphasis on receptor mechanisms and specific properties required for certain types of drugs in this respect. The book starts with some contributions dealing with various general aspects of drug kinetics followed by some contributions dealing with the relationship between certain physicochemical properties of drug molecules and their action. The text describes the pharmacokinetics and dose-concentration relationships; the time course of the biological response to drugs; and the empirical equations for correlating biological efficiency of organic compounds. The text also describes molecular basis for the action of chemotherapeutic drugs; the structure-activity studies on sulphonamides; and the water extrusion hypothesis. The mathematical treatment of two-point attachment between drug and receptor; the molecular properties and biological activity of catecholamines and certain related compounds; and the structure-activity relationships of diarylcarbinolethers are also considered. The book further tackles quantum mechanically-derived electronic distributions in the conformers of 2-pam; and the molecular basis for the action of certain drugs in the central nervous system. Pharmacologists and chemists will find the book invaluable.

Drug Design, Volume II covers the design of bioactive compounds interacting with enzymes and playing a role in enzyme synthesis. The book discusses the modulation of pharmacokinetics by molecular manipulation; the factors in the design of reversible and irreversible enzyme inhibitors; and the design of organophosphate and carbamate inhibitors of cholinesterases. The text also describes the design of reactivators for irreversibly blocked acetylcholinesterase; drug design based on the inhibition of protein synthesis in the context of susceptible enzymic reactions; as well as the role of enzymes and their synthesis as a target for antibiotic action. The rational design of antiviral agents; the design of penicillin; the design of peptide hormone analogs; as well as the advances in the design of diuretics are also considered. The book further tackles the design of biologically active steroids; the rational elements in the development of superior neuromuscular blocking agents; and the design of tumor-inhibitory alkylating drugs. Pharmacologists, chemists, and people involved in drug design will find the book invaluable.

Drug Design, Volume III covers the mode of action of biologically active compounds. The book discusses microbial transformations that have been used in the preparation of drugs or closely related substances; the use of linear free energy parameters and other experimental constants in structure-activity studies; and the mode of action of anticoagulants structurally and functionally related to vitamin K. The text also describes the design of beta-blocking drugs, biologically active acridines, local anesthetics, and insect chemosterilants. The molecular approach for designing inhibitors to enzymes involved in blood clotting is also considered. Chemists, pharmacologists, and people involved in drug design.

Drug Design, Volume IV covers the pharmaceutical phase of drug action, with emphasis on those aspects that are of importance in the design of optimally effective drug products. The book discusses biopharmaceutics as a basis for the design of drug products; the types and pharmacokinetics of peroral prolonged action dosage forms and parenteral prolonged action forms; and the design of topical drug products. The text also describes physical-chemical parameters which affect the bioavailability of topical drug products; the design of sunscreen preparations; as well as the clinical application of litholytic agents, which are preventive and curative drugs for nephrolithiasis. The design of biologically active nucleosides and of insecticidal chlorohydrocarbon derivatives is also encompassed. Chemists, biochemists, pharmacologists, and people involved in drug design will find the book invaluable.

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.

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.

Drug Design, Volume VII covers the design of agents such as blood substitutes, pesticides derived from insect pheromones, and herbicides related to the auxin-type plant hormones. The book discusses the design of artificial blood substitutes and auxin-type herbicides; the use of insect pheromones as a basis for the development of more effective selective pest control agents; and the development and application of new steric substituent parameters in drug design. The text also describes the use of computer technology in drug design. Pharmacologists, chemists, biochemists, and people involved in drug design and manufacture will find the book invaluable.

Drug Design, Volume VIII covers a critical review and new extensions of quantitative methods in drug design, the design of particular types of agents, such as synthetic sweeteners, and selective ion binding compounds. The book discusses the advances in the methodology of quantitative drug design; the application of pattern recognition to drug design; and the design of controlled drug delivery systems. The text also describes the use of receptor binding as a tool in the development of new bioactive steroids; the design of synthetic sweeteners; and the prospective assessment of environmental effects of chemicals. The design of selective ion binding macrocyclic compounds and their biological applications are also encompassed. Chemists, pharmacologists, biochemists, and people involved in drug design and manufacture will find the book invaluable.

Drug Design, Volume X covers promising and current developments in drug design. The book discusses procedures as applied in the practice of drug design; the structural aspects of the structure-activity relationships of neuroleptics; and promising perspectives in the highly actual field of bioactive peptides. The text also describes the application of the dynamic systems analysis to the antihypertensive drug action; polymeric drug delivery systems; and the design of biocompatible polymers. The structure-activity relationships of insect repellents as a basis for the design of such agents, as well as the approaches to the multivariate data analysis in structure-activity relationships, which is an essential aspect of drug design, are also encompassed. Chemists, pharmacologists, bioengineers, and people involved in drug design and manufacture will find the book invaluable.