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Focused efforts have been made to increase local-to-systemic activity ratios of potent anti-inflammatory steroids for local and/or topical applications. The approach taken in the present investigation is based upon the concept of "antedrug," defined as a locally active compound that exerts its
The effect on topical antiinflammatory potency of altering the ester functions of 7-halogenocorticosteroids was examined. Highest potencies for both 7 alpha-chloro- and 7 alpha-bromo-16 alpha-methylprednisolones were generally achieved through diesterification at the 17- and 21-positions. However,
Novel steroidal antiinflammatory antedrugs, 11 beta,20-dihydroxy-3,20-dioxo-3'-(ethoxycarbonyl)-isoxazolino[16,17 - d]pregna-1,4-diene (2a) and 9-fluoro-11 beta,20-dihydroxy-3,20-dioxo-3'-ethoxy- carbonylisoxazolino[16,17-d]pregna-1,4-diene (2b) were prepared in 97% yield via 1,3-dipolar
In a previous study, we analysed the synthesis and properties of a series of imidazo[1,2-alpha]quinoxalines designed in our laboratory as possible imiquimod analogues. We found that these imidazo[1,2-alpha]quinoxalines were in fact potent inhibitors of phosphodiesterase 4 enzymes (PDE4). PDE4
A recently developed compound, a multivalent guanylhydrazone (CNI-1493) that inhibits TNF-alpha production by suppressing TNF-alpha translational efficiency, was administered in an experimental model of collagen type II-induced arthritis in DA rats. CNI-1493 was injected daily intraperitoneally
Cardiovascular disease (CVD) is the leading cause of morbidity and mortality in the western world. Its incidence has been increasing lately in the developing countries. Much evidence suggests a major role for inflammation in all phases of atherosclerosis. Cell adhesion molecules, cytokines,