Chemistry
Early SEGRAs were synthetic steroids. An example is RU 24858, one of the first compounds of this type to be published. Many newer SEGRAs have a different framework, although the similarity to steroids can still be seen in molecules like the benzopyranoquinoline A 276575 or in octahydrophenanthrene-2,7-diol derivatives. All of these compounds have been shown to exhibit SEGRA properties in cellular or in animal models.
Mapracorat is one of a number of trifluoropropanolamines and -amides which are less obviously steroid-like in structure. Other typical examples of this group are ZK 216348 and 55D1E1. The bulky, bicyclic aromatic substituents (R1 and R2) account for the structural similarity to corticoids. The R conformation of the asymmetric carbon atom seems to be essential for GR affinity.
Read more about this topic: Selective Glucocorticoid Receptor Agonist
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