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"Many times drugs work fine when tested outside the body, but when they are tested in the body they fail. One of the major reasons a drug fails is that it cannot be absorb by the body in a way to have the effect it was intended to have. Permeability, solubility, dissolution, and charged state of ionizable molecules :- Helps drug discovery professionals to eliminate poorly absorbable molecules early in the drug discovery process, which can save drug companies millions of dollars.- Extensive tabulations, in appendix format, of properties and structures of about 200 standard drug molecules.This book attempts to describe the state of the art in measurement of ionization constants (pKa), oil–water partition coefficients (log P/log D), solubility, and permeability (artificial phospholipid membrane barriers). Permeability is covered in considerable detail, based on a newly developed methodology known as parallel artificial membrane permeability assay (PAMPA)."

"The essentials of drug metabolism vital to developing new therapeutic entities.Information on the metabolism and disposition of candidate drugs is a critical part of all aspects of the drug discovery and development process. Drug metabolism, as practiced in the pharmaceutical industry today, is a complex, multidisciplinary field that requires knowledge of sophisticated analytical technologies and expertise in mechanistic and kinetic enzymology, organic reaction mechanism, pharmacokinetic analysis, animal physiology, basic chemical toxicology, preclinical pharmacology, and molecular biology. With chapters contributed by experts in their specific areas, this reference covers :- Basic concepts of drug metabolism- The role of drug metabolism in the pharmaceutical industry- Analytical techniques in drug metabolism- Common experimental approaches and protocolsDrug metabolism in drug design and development emphasizes practical considerations such as the data needed, the experiments and analytical methods typically employed, and the interpretation and application of data. Chapters highlight facts, common protocols, detailed experimental designs, applications, and limitations of techniques."

"The medical benefits of a drug are not only dependent on its biological effect, but also on its "life cycle" within the organism, from its absorption into the blood, distribution to tissue until its eventual breakdown or excretion by the liver and kidneys.Here, the authors, all of them employed at Pfizer in the discovery and development of new active substances, discuss the significant parameters and processes important for the absorption, distribution and retention of drug compounds in the body, plus the potential problems created by their transformation into toxic byproducts. The authors cover everything from the fundamental principles right up to the latest developments using high throughput methods to analyze the pharmacokinetic properties of active substances.Particular emphasis is placed on the impact of pharmacokinetic parameters on the discovery of new drugs, one of the most challenging tasks in global pharmaceutical research."

"This book covers the science and approaches of enzyme inhibition applied in drug discovery and drug development, including both pharmacology and pharmacokinetic aspects of enzyme inhibition. Additionally, the book covers the inhibition of drug metabolizing and disposition enzymes including transporters (mostly "bad" or "undesirable" enzyme inhibition) as well as the inhibition of drug target enzymes (mostly the "good" or "desirable" enzyme inhibition). Each chapter details the basic scientific concepts, experimental approaches, data interpretation, and current challenges and promising advancements for a specific type of inhibition."

"Born out of a project of the IUPAC's committee on Medicinal Chemistry and Drug Development, this reference addresses past and current strategies for successful drug analog development, extending the previously published volume by nine new analog classes and eight case studies. Like its precursor, this volume also contains a general section discussing universally applicable strategies for analog discovery and development. Spanning a wide range of therapeutic fields and chemical classes, the two volumes together constitute the first systematic approach to drug analog development."

"The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds. Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them. The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability."

"This resource provides an integrated and comprehensive overview of modern approaches to drug lead discovery. Each chapter in this book reviews the theoretical background and application of a key technology in drug discovery, complemented by relevant case studies. The coverage includes the key approaches for drug design and discovery, high-throughput screening, fragment screening, multi-target drugs, de novo design, ADMET, natural products. This cutting-edge reference helps medicinal chemists in biotech, pharmaceutical, and other research contexts consider all possible avenues in starting their drug research programs."

"Explaining the assessment of potential drug compounds, this is an ideal introductory reference for those new to drug discovery. It includes sections on pharmacokinetics and drug metabolism, integration of pharmaceutical development, and predictive safety assessment. Topics include: cost analysis, drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, assessing stability, ways to optimize drug formulation, toxicology and toxicokinetics, and more. Readers will understand why absorption-distribution-metabolism-excretion-toxicology (ADMET) is key in drug development. "