Dmgs of Inflammatory and Immunity Disorders

Glucocorticoids are important metabolic hormones with a central role and many implications. They interact with nuclear receptors. The latter act on transcription factors of the genes coding proteins that are involved in the control of inflammation. 

Betamethasone (Lederle) 1956 R = H, acetate, propionate phosphate, valerate, etc. 

Dexamethasone (Merck) 1957 21 = acetate, palmitate, phosphate pivalate, isonicotinate etc. 

Fluorination of corticosteroids at C-9 or/and C-6 increases glucocorticoid activity, while mineralocorticoid activity, responsible for sodium retention (the main adverse effect of corticoids), is decreased (cf. Chapter 4). Fluorocorticoster-oids were the first fluorinated compounds to be used clinically. They are still major drugs against many inflammatory disorders rheumatoid polyarthritis, ORL (asthma, rhinitis), brain edema, dermatological, allergies, anaphylactic shock, Quincke s edema). 

A substitution can be made with another halogen at C-2 halomethasone, halo-predone) or at 21 (21-OH 21-Cl) clobetasol, halobetasol). Fluclorolone is an 

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