Historical perspective medicinal chemistry

The various topics discussed in this book have up to this point been arranged as far as possible on the basis of chemical structure compounds that contain one oxygen and one nitrogen atom have, for example, as a general rule preceded those that contain two nitrogen atoms. The fact that virtually all of the entities that follow show CNS activity combined with the circumstance that phenothiazines comprise a large part of this section require a departure from that approach. The serendipitous discovery of the antipsychotic activity of the phenothiazines in the early 1950s virtually opened the modern era of medicinal chemistry. These will thus be discussed at the outset to preserve historical perspective. 

Since the appearance of computer-aided structure-activity studies, the term pharmacophore has become one of the most popular words in medicinal chemistry. However, depending on their scientific background and/or traditions, the different medicinal chemistry groups attribute various meanings to this term. Therefore, it appeared necessary to devote a brief paragraph to the definition of the word pharmacophore, and this is followed by a historical perspective and finally by some comments from a medicinal chemistry practitioner. 

Hansch, C., Selassie, C. Quantitative structure—activity relationship — a historical perspective and the future. In Comprehensive Medicinal Chemistry 2 Ed., vol. 4, Computer-Assisted Drug Design, (Taylor, J. B., Triggle, D. J., Eds), Elsevier Oxford, 2007, pp. 43-63. 

Erhardt, P. W., Sc Proudfoot, J. R. (2006). Drug discovery—Historical perspective, current status and outiook. InJ. Taylor Sc D. Triggle (Eds.), Comprehensive Medicinal Chemistry (Vol. 1). Oxford, United Kingdom. 

The review provides an overview of the chemistry and pharmacology of the most relevant and investigated compounds, contrasting the current biomedical knowledge with the concepts and practices in the XVI century medicine. The authors use historical materials in combination with phytochemistry and pharmacology to provide an incentive to the new generation of natural product scientists to maintain a broad perspective in their field of scientific inquiry. Also to the young scientists is our hope is to convey appreciation and historical perspective of science and cultural diversity. 

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