Chemistry

JOS√ČE SCHEPPER

Research Library and Information Centre, Merck Frosst Canada & Co., Kirkland, Quebec, Canada

Medicinal chemistry is the field of chemistry dealing with the discovery and design of new chemicals (drugs) used as therapeutic agents to treat diseases. In the drug discovery process, when a new compound or molecule is isolated or synthesized, it is referred to as a new chemical entity (NCE).

The road from NCE to new drug application (NDA) is a long one. Researchers first have to prove that the compound is nontoxic and can demonstrate the desired therapeutic effect in animal models. If those results are promising, they then have to apply to the Food and Drug Aministration (FDA) for permission to begin testing the compound in humans. After years of clinical trials, the new compound may eventually become a new medicine on the market. NCEs may be derived

from natural compounds, which are subsequently modified to improve therapeutic characteristics, or they may be developed in the laboratory via chemical synthesis. Medicinal chemistry is the study of the biological activity of compounds, their interactions with enzymes and receptors, and their actions in metabolic transformations. These studies examine the molecular level of drug interactions and are the crucial first steps in isolating potential NCEs.

Medicinal chemists also study the activation of "prodrugs." A prodrug is a pharmacologically inactive molecule that is converted into an active compound by the body's metabolism. This strategy is used to get around the potential obstacles to drug delivery in the body, such as poor absorption or instability. Knowledge of how a particular compound interacts with metabolic processes is key when designing safe and effective drugs.

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