Glucocorticoid structure-activity relationship

Most glucocorticoids have some mineralocorticoid effect, which is usually considered an undesirable activity. Through structural chemistry and structure-activity relationship (SAR) studies, molecular modifications can separate the two activities. 

The structure-activity relationships of glucocorticoids are based on two natural hormones, cortisol (3.8) and corticosterone (5.61). The characteristic structural features of these hormones are the conjugated 3-ketone, the 11-OH group, and the up-ketol side chain. Molecular modifications have been aimed at deriving compounds with glucocorticoid... 

Johansson M, Earsson C, Bergman A, et al. 1998. Structure-activity relationship for inhibition of CYPl IB 1-dependent glucocorticoid synthesis in Yl cells by aryl methyl sulfones. Pharmacol Toxicol (Amsterdam) 83 225-230. 

Structure-Activity Relationship (SAR) Intensive and extensive clinical investigations have duly revealed that the anti-inflammatory activity emanated by the adrenal cortical steroids in humans invariably correlates intimately with their respective glucocorticoid activity. The advent of glaring and outstanding researches have evolved several synthetic steroids that exclusively possess distinctly higher glucocorticoid, and relatively lower mineralocorticosteroid activity in comparison to cortisone or cortisol that have been duly prepared, biologically screened, and marketed. 

Miscellaneous Activity - In the corticoid area, several C21 derivatives of known active corticoids were prepared and evaluated. " A new non-halogenated glucocorticoid possessing "extraordinary anti-inflammatory potency" was reported,8 and the pharmacology of 9ct-fluorohydrocortisone was extensively reviewed.The relationships between structure and... 

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