Drug discovery learning experiences

In fall 2001, I taught medicinal chemistry for the first time. My training is in synthetic organic chemistry, and I learned many of the class topics about a week before my students. In summer 2002, I attended the Residential School on Medicinal Chemistry at Drew University. The Drew course was a fantastic experience. For me, the value of the course was less about the material and more about seeing practitioners of medicinal chemistry talk about the drug discovery process in their own language. In this textbook, I have tried to be true to the ideas and attitudes that seem inherent to those who are actively involved in the pharmaceutical industry. 

Dr William Jorgensen, a professor at Yale with many years of experience in computational drug discovery, reflects on a question often posed to such researchers, Is there really a case where a drug that s on the market was designed by computer When asked this, he notes, I invoke the professorial mantra ( All questions are good questions. ), while sensing that the desired answer is no . Then, the inquisitor could go back to the lab with the reassurance that his or her choice to avoid learning about computational chemistry remains wise. ... 

Prontosil is an effective antibacterial substance in vivo, that is, when injected into a living animal. Prontosil is not medicinally active when the drug is tested in vitro, that is, on a bacterial culture grown in the laboratory. In 1935, the research group at the Pasteur Institute in Paris headed by J.Tr fouel learned that Prontosil is metabolized in animals to sulfanilamide. Sulfanilamide had been known since 1908. Experiments with sulfanilamide showed that it had the same action as Prontosil in vivo and that it was also active in vitro, where Prontosil was known to be inactive. It was concluded that the active portion of the Prontosil molecule was the sulfanilamide moiety. This discovery led to an explosion of interest in sulfonamide derivatives. Well over a thousand sulfonamide substances were prepared within a few years of these discoveries. 

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