I1 Medicinal Chemistryan Interdisciplinary Science

Therapeutic agents are chemicals that prevent disease, assist in restoring health to the diseased, or alleviate symptoms associated with disease conditions. Medicinal chemistry is the scientific discipline that makes such drugs available through either discovery or design processes. Throughout history, drugs were primarily discovered by empirical methods, investigating substances or preparations of materials found in the local environment. Over the previous centuries, chemists developed methods and techniques for the isolation and purification of the active principles in medicinal plants. The purification and structure determination of natural products like morphine, hyoscy-amine, quinine, and digitalis glycosides represent milestones in the field of drug discovery and the beginning of medicinal chemistry as a fascinating independent field of research (Figure I.1).

In the twentieth century, a very large number of biologically active natural products were structurally modified in order to optimize their pharmacology, and novel drugs were prepared by use of increasingly advanced synthetic methods. Moreover, the rapidly growing understanding of the nature of disease mechanisms, how cells function, and how drugs interact with cellular processes has led to the rational design, synthesis, and pharmacological evaluation of new drug candidates. Most recently, new dimensions and opportunities have emerged from a deeper understanding of cell biology and genetics.

Modern medicinal chemistry draws upon many scientific disciplines, organic and physical chemistry being of fundamental importance. But other disciplines such as biochemistry, molecular biology, pharmacology, neurobiology, toxicology, genetics, cell biology, biophysics, physiology,

Morphine

Hyoscyamine

Quinine

Morphine

Hyoscyamine

Quinine

Digitoxin

FIGURE I.1 Chemical structures of four naturally occurring classical therapeutic agents.

Digitoxin

FIGURE I.1 Chemical structures of four naturally occurring classical therapeutic agents.

pathology, and computer technologies play important roles. The key research objective of medicinal chemistry is to investigate relationships between chemical structure and biological effects. When the chemical structure of a particular drug candidate has been optimized to interact with the biological target, the compound further has to fulfill a multifaceted set of criteria before it can be safely administered to patients. Absorption-distribution-metabolism-excretion (ADME) and toxicology studies in animals and humans are time-consuming research tasks, which often call for redesign of the chemical structure of the potential therapeutic agent investigated. It is an iterative process that is bound to end up in an overall compromise.

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