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An examination of the important role of fluorine in medicinal chemistry reveals that, in most cases, an organic compound needs be only lightly substituted with fluorine. Indeed, a single fluorine atom or a trifluoromethyl group, located in a key position of a bioactive molecule, can exert a profound pharmacological effect. Recently, developments in previously well-studied fields have been augmented by exciting reports in newer areas. The topics chosen by the authors are likely to be of broad interest and represent the work of established international leaders in their areas of research. Keeping in mind the question "what does fluorine provide that is so special?", the reader will find information on anticancer and antiviral agents and be brought up to date on volatile anesthetics and central nervous system agents, areas in which fluorine has played a pivotal role for almost 40 years. Antibiotics receive special attention, with coverage of beta-lactams and fluoroquinolone antibacterials.Newer applications of biologically-active fluorine compounds are reviewed, including cardiovascular drugs, fluoroamino acids and peptides, and the prostaglandins and leukotrienes of the arachidonic acid cascade. Biomedical applications, such as 18F in positron emission tomography (PET) and fluorinated surfactants are well covered. In the opening chapter, an overview of the field is given, including brief reports on areas not otherwise covered in the book, eg. recent advances in antidiabetic and hypolipidemic agents. ... Read more

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Fullerenes and nanotubes are two classes of carbon structures or allotropes, which were discovered about 17 years ago. Since that time, many chemical derivatives have been synthesized using fullerenes and nanotubes as building blocks.

Particularly promising was the theory that the chemical properties of fullerenes, and certain derivatives, made them likely candidates for anticancer drugs, inhibitors of viruses such as HIV, or even as anti-bacterials. Their cyctotoxicity can also be controlled by specific circumstances.

In addition, the funtionalization of nanotubes has not only produced relatively simple derivatives, but also complex hybrids with biological macromolecules, which show unique supramolecular architecture and which are promising in many medical applications.

The application of fullerenes and nanotubes in medicine is at the frontier of our knowledge, thus the work in this field represents the basis for future novel developments.

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University of Karachi, Pakistan.First volume in a new series on the field of medicinal chemistry. Introductory volume reviews current research topics. 14 contributors, 2 U.S. ... Read more

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Medicinal or pharmaceutical chemistry is a scientific discipline at the intersection of chemistry and pharmacology involved with designing, synthesising and developing pharmaceutical drugs. Medicinal chemistry involves the identification, synthesis and development of new chemical entities suitable for therapeutic use. It also includes the study of existing drugs, their biological properties, and their quantitative structure-activity relationships (QSAR). Pharmaceutical chemistry is focused on quality aspects of medicines and aims to assure fitness for the purpose of medicinal products. Medicinal chemistry is a highly interdisciplinary science combining organic chemistry with biochemistry, computational chemistry, pharmacology, pharmacognosy, molecular biology, statistics, and physical chemistry. This book presents leading research from around the world in this frontal field. ... Read more

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The many new and fascinating data which have been gathered in the period 1985-1990 have made molecular endocrinology into a mature discipline stimulating creative chemists to design innovative drugs. Within a few years, the primary structures of all the steroid receptor proteins and most of the steroid-converting enzymes have been determined and detailed studies of their mechanism of action at a molecular level have become possible. Medicinal chemists have developed steroidal affinity probes to examine the binding sites of enzymes and receptors, and these investigations were supplemented with studies of modified enzymes and receptors prepared with the aid of site-directed mutagenesis. In view of these rapid scientific developments, the author deemed it appropriate to review the present knowledge of the medicinal chemistry of the steroids. In this book, the discussion is supported by the addition of some chapters which summarize the available data on the biological counterparts of the steroids, the steroid-converting enzymes and the steroid receptors. ... Read more

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Medicinal Chemistry Laboratory Manual: Investigations in Biological and Pharmaceutical Chemistry responds to a critical classroom need for material for directed laboratory investigations in biological and pharmaceutical chemistry. This manual supplies 55 experiments in 18 major subject areas, including carbohydrates, lipids, and proteins in biochemistry; tannins, balsams, and alkaloids in natural products areas; and analgesics, steroids, and anesthetics in pharmaceutical chemistry. ... Read more

Customer Reviews (1)

High School Independent Study
If you are looking for a book with ideas for activities and labs with a biological or pharmaceutical emphasis, I highly recommend this text/lab-manual.There are 18 chapters with a total of 55 lab exercises.Many exercises are isolations and purifications (Isolating Lactose from Milk, Isolation of Citric Acid from Lemon, Isolation of Alkaloids from Plant Sources, Steam Distillation of Peppermint Oil) others involve assays (Color Tests for Carbohydrates, Determining the Saponification Number of an Oil, Determining Vitamin C content in Commercial Tablets) others offer comparative tests (Chromatography of Alkaloids, Paper Chromatography of Amino Acids, Identification of Analgesics using TLC) while others offer experience in simple chemical syntheses (Synthesis of Acetylsalicylic Acid, Preparation of Acetominophen, Preparation of Sulfanilimide).

The variety of topics, the range of difficulty levels and the detailed instructions make this a top selection for my courses. ... Read more

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Barrier, reservoir, target site - those are but some of the possible functions of biological lipid membranes in the complex interplay of drugs with the organism. A detailed knowledge of lipid membranes and of the various modes of drug-membrane interaction is therefore the prerequisite for a better understanding of drug action. Many of today's pharmaceuticals are amphiphilic or catamphiphilic, enabling them to interact with biological membranes.
Crucial membrane properties are surveyed and techniques to elucidate drug-membrane interactions presented, including computer-aided predictions. Effects of membrane interaction on drug action and drug distribution are discussed, and numerous examples are given.
This unique reference volume builds on the authors' long experience in the study of drug-membrane interaction. Recommended reading for everyone involved in pharmaceutical research. ... Read more

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Medicinal or pharmaceutical chemistry is a scientific discipline at the intersection of chemistry and pharmacology involved with designing, synthesising and developing pharmaceutical drugs. Medicinal chemistry involves the identification, synthesis and development of new chemical entities suitable for therapeutic use. It also includes the study of existing drugs, their biological properties, and their quantitative structure-activity relationships (QSAR). Pharmaceutical chemistry is focused on quality aspects of medicines and aims to assure fitness for the purpose of medicinal products. Medicinal chemistry is a highly interdisciplinary science combining organic chemistry with biochemistry, computational chemistry, pharmacology, pharmacognosy, molecular biology, statistics, and physical chemistry. This book presents leading research from around the world in this frontal field. ... Read more

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The use of powerful computers has revolutionized molecular design and drug discovery. Thoroughly researched and well-structured, this comprehensive handbook covers highly effective and efficient techniques in 3D-QSAR and advanced statistical analysis. The emphasis is on showing users how to apply these methods and avoid costly and time-consuming methodical errors.

Topics covered include
* combination of statistical methods and molecular modeling tools
* rational use of databases
* advanced statistical techniques
* neural networks and expert systems in molecular design

This book addresses the practitioner in industry and research, as well as the novice wishing to become acquainted with modern tools in medicinal chemistry. ... Read more

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Transporters are proteins which span the plasma membrane and regulate the traffic of small molecules in and out of the cell. Transporters play a particularly important role in chemical signalling between neurons in the CNS, where they act to control the concentration of neurotransmitters in the synapse. The majority of transporters which are actively being pursued as targets for drug discovery are CNS located and this reflects the history of the field which began with the tricyclic antidepressants (TCAs) over half a century ago. The use of transporter inhibition to regulate the synaptic concentrations of key neurotransmitters is an established approach in the discovery of psychiatric medications. This volume reviews advances in the field of transporters as targets for drug discovery in the last 10 years. The volume will be of interest to scientists engaged in drug research in the pharmaceutical industry, biotech and academia. Following an overview chapter, seven chapters written by leading experts in their area reflect a range of topics pertinent to the transporter field. General topics include recent advances in the structural biology of transporters and its impact on potential structure based drug design and the design of ligands for Positron Emission Tomography and the importance of molecular imaging in understanding early clinical data. Medicinal chemistry approaches are described outlining the discovery of selective serotonin, noradrenaline and dopamine reuptake inhibitors, current efforts towards the discovery of mixed re-uptake inhibitors with varied ‘flavours’ of monoamine inhibition, advances in the development of inhibitors for the glycine transporter and the discovery of subtype selective EAAT inhibitors. In addition to being an interesting read, the reader will receive a critical overview of progress made in this rapidly developing field.

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This book contains topics that include: Overview of Hit to Lead: The Medicinal Chemist's Role from HTS Retest to Lead Optimization Hand Off (Christopher A. Lipinski); High Throughput Screening in the 21st Century (Jeff W. Paslay, John E. Morin, and Richard K. Harrison); Lead Discovery Using Virtual Screening (Jack Andrew Bikker and Lakshmi S. Narasimhan); NMR Spectroscopy in Fragment Based Drug Design (Maurizio Pellecchia); Hit Triage - Medicinal Chemistry Strategies to Improve the Odds of Success in Discovery (Kevin D. Freeman-Cook and Daniel W. Kung); and Lead Identification (John W. Ellingboe and Adam M. Gilbert). ... Read more

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This Second Edition covers exciting progress recently made with individual drugs and includes a special chapter on the impact of molecular biology on drug design.Other additions to the Second Edition include structure-activity relationships, the role of molecular biology in drug discovery, and drug access and prodrugs.Written for students considering a research career in drug development, this volume is conveniently divided into two parts.The first half introduces readers to the mechanisms of action of drugs and the approaches adopted in designing new drugs.The second half contains chapters written by the discoverers or developers of individual successful drugs who trace the history of the drugs to the present day.
... Read more

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Significant advances in genomics have provided a plethora of previously unknown molecular targets, and with it the opportunity to discover and develop a variety of important new medicines.The timely and successful exploitation of these targets, however, has presented scientists with an appreciable challenge.New, efficient lead generation paradigms, resulting in increasingly large and diverse chemical libraries, have driven the technological advances needed to support their design, characterization and analysis. Bringing together contributions from international experts in both industry and academia, "Medicinal Chemistry into the Millennium" reports on a number of important developments.Subjects covered include many of the newer supporting technologies and the specific challenges posed by the need to predict bioavailability characteristics.The application of these techniques in the exploitation of targets as diverse as grown factors, proteases, 7-transmembrane receptors, ion intracellular signalling processes, is also discussed. The topics covered in this book are particularly relevant to scientists in the pharmaceutical industry and other industries dependent on the discovery of biologically active molecules. ... Read more

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Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies. ... Read more

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This first systematic overview for more than a decade is tailor-made for the medicinal chemist. All the chapters are written by experienced drug developers and include practical examples from real drug candidates. Following an introduction to global drug properties and their impact on drug research, screening and combinatorial chemistry libraries, this handbook demonstrates the best and fastest way to estimate those properties most relevant for the efficiency and pharmacokinetic performance of a drug molecule: lipophilicity,solubility, electronic properties and conformation. ... Read more

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Medicinal Chemistry: Today and Tomorrow presents theedited proceedings of the AFMC International Medicinal ChemistrySymposium. Medicinal chemistry is an interdisciplinary sciencecovering a broad range of subjects but with chemistry as its core. Thegoal of medicinal chemistry is to produce effective newpharmaceuticals. The subject has seen remarkable advances in recentyears, and Medicinal Chemistry: Today and Tomorrow provides asynthetic overview of the state of the art. This volume should make animportant contribution to medicinal chemistry in its quest to produceinnovative drugs that make the best use of recent developments inpharmaceutical research. ... Read more

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A broad overview of the latest advances in medicinal chemistry.

Emphasis is placed on
- drug design
- new therapeutic agents
- treatment of major diseases, such as AIDS and malaria.

The book discusses recently discovered targets for drug action. It also takes a look at the theoretical and experimental tools which have fostered our understanding of the molecular mechanisms of drug action. ... Read more