Prednisolone

Nonsteroidal Selective Glucocorticoid Modulators: The Effect of C-10 Substitution on Receptor Selectivity and Functional Potency of 5-Allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines

“…Having long been considered among the most potent anti-inflammatory agents known, oral glucocorticoids such as dexamethasone (dex, 1 ) and prednisolone (pred, 2 ) continue to represent the clinical gold standard for treatment of numerous musculoskeletal, respiratory, gastrointestinal, and dermatological disorders. − Unfortunately, these beneficial anti-inflammatory and immunomodulatory effects are counterbalanced by a broad spectrum of adverse events, the frequency and severity of which tend to increase with increased dosage, length of therapy, and systemic exposure. These deleterious side effects, which include osteoporosis, glucose intolerance, lipid redistribution, and acute psychosis, have limited a more widespread therapeutic use of synthetic glucocorticoids.…”

A Practical and Scaleable Synthesis of A-224817.0, a Novel Nonsteroidal Ligand for the Glucocorticoid Receptor

“…Glucocorticoids therapy has been used for the treatment of inflammatory diseases for more than forty years. Synthetic glucocorticoids such as dexamethasone and prednisolone have been widely used in the clinical treatment of chronic inflammatory diseases. It is also well documented that corticosteroid antiinflammatory therapy causes many undesirable side effects, such as glucocorticoid-induced osteoporosis and glucose intolerance…”

Synthesis and Characterization of Non-Steroidal Ligands for the Glucocorticoid Receptor: Selective Quinoline Derivatives with Prednisolone-Equivalent Functional Activity

“…The endogenous members of this family, cortisol and cortisone (Chart ), are involved in a broad spectrum of endocrine functions including metabolism of lipids, carbohydrates, and proteins, stress response, fluid and electrolyte balance, as well as maintenance of immunological, renal, and skeletal homeostasis. − Prompted by the isolation of GCs and identification of their structures in the mid 1930s, a monumental research effort in the 1940s and 1950s resulted in the discovery of newer, more potent analogues and an understanding of their biological properties, especially antiinflammatory effects. Prednisolone and dexamethasone emerged as benchmark drugs during this era. Although GCs are associated with a variety of clinical side effects, they are used for a breadth of antiinflammatory therapies while the search has continued for newer, more selective analogues.…”