2024-03-05 23:00:00
Certain functional groups carry biological activity and confer this activity with a highly significant frequency to the molecules onto which they can be grafted. For example, alcohols and phenols exhibit sedative and antiseptic effects, respectively, while the bis-(2-chloroethylamine) motif, found in several anticancer agents such as chlorambucil, is responsible for their alkylating properties. In the same way, cyclic skeletons, such as the cyclopentanoperhydrophenantric chain, constitute the common motif of steroids with hormonal, anti-inflammatory, diuretic and cardiostimulating activity.
Thus, particular structural elements, grouped under the term pharmacophore, are recognized by a target, receptor or enzyme, and responsible for biological activity. The substituents fixed on these pharmacophores only intervene to modulate the activity and/or to modify the pharmacokinetics of the active ingredients: increase in the duration of action, reduction in toxicity, improvement in bioavailability, increase in stability, etc.
The qualitative structure-activity relationships, originally established empirically from the analysis of the formulas of the active ingredients, were reinforced then developed thanks to molecular modeling studies, to become essential in the context of the design of new drugs (drug design).
The objective of this article is to first learn to recognize the main structural motifs vectors of pharmacological activity, based on active ingredients characteristic of the main families of drugs currently on the market. Secondly, the fundamental mechanisms of action of each therapeutic class are discussed in connection with the skeletons of the active substances.
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