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For many years, Burger's Medicinal Chemistry and Drug Discovery has been considered the landmark reference text for medicinal chemists. The new sixth print edition of this series, which consists of more than pages spanning 6 volumes, is a Memorial Edition to Professor Alfred Burger. Burger, one of the early academic scientists to design and synthesize a compound in his laboratories that was subsequently brought to market, first published this major reference work in as the 2 volume set Medicinal Chemistry. In its latest iteration, Burger's Medicinal Chemistry and Drug Discovery, Sixth Edition has been expanded and updated to include many new topics relevant to medicinal chemists, including proteomics, genomics, bioinformatics, combinatorial chemistry and high-throughput screening, blood substitutes, allosteric effectors as potential drugs, COX inhibitors, statins, and high-throughput pharmacology.

In this form, the text and all associated figures and tables are available in HTML format, lending a degree of portability to an otherwise non-transportable reference source.


As outlined below, each of the 6 volumes is divided into chapters revolving around a major theme eg, Chemotherapeutic Agents. Each chapter is written by one or more recognized experts in a given field of research, and the material is presented at the level of a comprehensive research review. Thus, the content is of great value for researchers in medicinal chemistry, but is not generally suitable for undergraduate students. Each chapter has between and references to the primary literature, a major strength of this reference text, making this series a valuable tool for anyone conducting research in medicinal chemistry.

In many cases, authors have also provided references to sites on the World Wide Web where additional information can be sought. Individual chapters provide an overview of the biochemical and pharmacological basis for an area of research, the history of the design and development of novel drug molecules, and the most recent advances in the field.

The text is replete with tables, illustrations and structures that complement the text and serve to illustrate major points. One perceived weakness of the series is that there seem to be several different formats for chapters, and internal numbering systems within a chapter can be confusing eg, Section 6. Also, in some cases, structures appear within numbered figures, while in other chapters, structures appear individually with sequence numbers that are referenced in the text.


However, the style is consistent within each individual chapter and these anomalies detract minimally from the readability of the text. The topics covered in each thematic volume of the series are outlined below. A comprehensive description of each volume is beyond the scope of this review, but the content of each individual volume is briefly described:. Volume 1: Drug Discovery. Volume 1 of the Burger series contains 20 chapters that deal with various practical and theoretical aspects of medicinal chemistry and drug discovery.

The topics covered are general, and techniques are stressed globally, rather than as they relate to a specific therapeutic area. Chapter 3 provides a comprehensive review of the theoretical aspects of molecular modeling, and describes the use of these principles for the design of ligands for known and unknown receptors, while the fourth chapter outlines the theoretical aspects of binding forces and the development of force field equations for molecular mechanics. Chapter 5 deals with the design of combinatorial libraries and screening of candidates based on molecular similarity and diversity, while chapter 6 discusses virtual screening methods, including pharmacophore screening and other in silico techniques.

This is immediately followed by a chapter dealing with docking and scoring techniques for computer-assisted drug design. Also included are excellent chapters covering principles of bioinformatics Chapter 8 and the use of computerized chemical information systems Chapter 9. Thus the first 9 chapters provide an authoritative primer on the theoretical aspects of computer-assisted drug design and data management.

Abraham, D. — Rotella, D.

Beginning with Chapter 10, volume 1 discusses aspects of structure-based drug design, and provides chapters outlining the use of X-ray crystallography Chapter 11 , NMR Chapter 12 , mass spectroscopy Chapter 13 and electron microscopy Chapter 14 in the design of new drug entities. More traditional topics are covered in subsequent chapters, such as peptidomimetics, analog design, enzyme inhibition, chirality, drug toxicity, and the use of natural products as leads for drug discovery. Each of these chapters is written in sufficient detail to give a comprehensive overview of the techniques involved in each endeavor.

Volume 2: Drug Discovery and Drug Development. Volume 2 continues on the theme of describing modern drug discovery methodology. Chapters 1—3 are reviews of combinatorial synthesis, high throughput screening, and high throughput pharmacology, respectively.

Burger's Medicinal Chemistry, Drug Discovery and Development, 8 Volume Set

Together, these chapters provide an excellent overview of the process of rapid drug discovery in the pharmaceutical industry. The next 6 chapters deal with biotechnology-related topics such as recombinant DNA technology in drug design, oligonucleotide therapies, agents with RNA targets, carbohydrate-based therapeutics, drug transport proteins, and allosteric effectors as drugs. Chapter 10 provides a complete description of receptor-targeting strategies, including an overview of molecular pharmacology principles, and Chapter 11 provides a review of the structure and function of the nicotinic acetylcholine receptor, including the pharmacology of nicotinic agonists and antagonists.

The following chapters 12—20 contain reviews of practical methodologies pertinent to drug development, including large-scale synthesis, drug metabolism, prodrug design, toxicology, ADME, dosage form selection, a description of the role of the FDA in the drug development process, and management of intellectual property. Volume 3: Cardiovascular Agents and Endocrines. In volumes 3—6, the Burger series undertakes the description of drug entities according to therapeutic class; volume 3 is dedicated to drugs with effects on the cardiovascular and endocrine systems.

The chapters in this volume are arranged in a manner similar to a standard medicinal chemistry text aimed at pharmacy students, but the material is in much greater depth, and includes agents that are experimental in nature. Chapters in volume 3 are dedicated to traditional agents such as antianginal agents, vasodilators, diuretics and uricosurics, agents for the treatment of myocardial infarction, hematopoietic agents, vasoactive peptides, anticoagulants, antihyperlipidemic agents, thyroid hormones, steroids, male and female sex hormones, and anti-inflammatory agents.

Also included are chapters on more nontradional subjects such as allosteric effectors of hemoglobin as oxygen delivery aids, blood substitutes, plasma extenders, treatment of sickle cell anemia, and metal chelators. As was the case with volume 3, chapters in this volume are analogous to a standard medicinal chemistry text, but are in much greater depth. Each topic is completely reviewed with respect to underlying biochemistry and pharmacology, history of drug development, and current status of ongoing research in the area.

Chapters deal with material that is more traditional in nature insulin, peptide hormones, neurotransmitters, inhibitors of gastric acid secretion, vitamins as well as some more recent areas of medicinal chemistry research chemokines, COX-2 inhibitors, prostaglandins, retinoids, radioopaque agents.

Chapters on lifestyle and over-the counter drugs, microarrays and gene expression, single nucleotide polymorphisms and gene therapy, which provide insight into emerging areas of medicinal chemistry, are also included. Volume 5: Chemotherapeutic Agents. Volume 5 of this series is dedicated to a comprehensive description of chemotherapeutic agents, and is roughly divided between chapters dealing with cancer chemotherapy Chapters 1—8 and antiinfective agents Chapters 9— Like volumes 3 and 4, volume 5 presents material within a given topic area, from basic concepts up to the research level, including the most recent trends and examples of experimental agents.

Chapter 1 is an outstanding review of the molecular biology of cancer, as well as the cellular processes involved in carcinogenesis. Subsequent chapters then discuss DNA-targeted antitumor agents, natural products as antitumor agents, radiosensitizers and radioprotective agents, antiangiogenic agents, immunotherapy, selective toxicity, and drug resistance in cancer chemotherapy. Volume 6: Nervous System Agents. Volume 6 of the Burger series is quite analogous to a traditional medicinal chemistry text, except that the material is covered in much greater depth, and in most cases recent trends in a given area are reported.

Tradional classes such as adrenergics, cholinergics, anticholinergics, CNS stimulants, sedative hypnotics, anticonvulsants, narcotic analgesics, antidepressants, antianxiety agents, drugs for the treatment of Parkinsonism, and antipsychotic agents are covered in this volume, largely in the format mentioned above. The chapter on narcotic analgesics is exceptionally complete, discusses the most recent research trends in the area, and contains over references to the primary literature.

Where appropriate in each chapter, a discussion of the most recent studies dealing with receptor structure and function are included. Four additional chapters cover some of the more recent topics in medicinal chemistry research, including agents for neurodegenerative disease, drugs for the treatment of Alzheimer's disease, cognition enhancers, and antiobesity drugs. In summary, Burger's Medicinal Chemistry and Drug Discovery, Sixth Edition , is an up-to-date and comprehensive compendium of modern research in medicinal chemistry.

Alfred Burger's internationally celebrated classic helps researchers acquaint themselves with both traditional and state-of-the-art principles and practices governing new medicinal drug research and development. Completely updated and revised to reflect the many monumental changes that have occurred in the field, this latest edition brings together contributions by experts in a wide range of related fields to explore recent advances in the understanding of the structural biology of drug action, as well as cutting-edge technologies for drug discovery now in use around the world.

To purchase the entire 6 volume set, please refer to ISBN For a complete list of articles and contributors as well as FREE sample chapters from this new 6th Edition please visit the online edition at: www.

Congestive Heart Failure. Endogenous vasoactive peptides.

  • Copyright:.
  • T Cell Activation by CD1 and Lipid Antigens.
  • Nonlinear Dynamics: A Primer.
  • Introduction to Artificial Neural Systems.
  • Systems Biology of Alzheimers Disease.

Hematopoietic agents. Oxygen delivery via allosteric effectors of hemoglobin and blood substitutes. Fundamentals of steroid chemistry and biochemistry. Antiinflammatory Glucocorticoids. Male sex hormones, analogs, and antagonists.

Female Sex Hormones pick up from the online. Multiple sclerosis. Ophthalmic agents. Osteoporosis therapy: mechanistic antiresoptives. Osteoporosis therapy: anabolics. Therapeutic agents acting on RNA. Immunosuppressive agents for the prevention of transplantation rejection. Volume 6: Cancer.

Natural product cytotoxics. Histone Deacetylase Inhibitors: A brief overview of their role and medicinal chemistry. Synthetic DNA-targeted chemotherapeutic agents and related tumor-activated prodrugs. Proteasome inhibitors. CNS Cancers. Kinase inhibitors: Approved Drugs and Clinical Candidates.

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Cancer drug resistance-targets and therapies. HSP inhibitors. Gene therapy with plasmid DNA. Volume 7: Antiinfectives. HIV integrase. CCR5 Antagonists.