Synthesis of lipoxygenase inhibitors. Part 2: Synthesis of lactamarylhydrazones and tetrahydroazepinochinazolinon-arylhydrazones
The synthesis of lactamarylhydrazones as cyclic amidrazones is described starting from 5-, 6- and 7-membered lactames. Tetrahydroazepinochinazolinonarylhydrazones were prepared from caprolactam. The compounds were tested against soja lipoxygenase. A few compounds were very strong inhibitors (IC50 value up to 4.10-9 mol/l).
Composition comprising an oxygenated cholesterol and use thereof for topical treatment of diseases
The invention is directed to a pharmaceutical composition comprising an oxygenated cholesterol and a penetration-enhancing agent which is useful for topical application to the skin of a patient suffering from a proliferative skin disease characterized by geminative cells having a rapid rate of replication, e.g. psoriasis. The composition comprises an effective amount for the inhibition of germinative cell mitosis of an oxygenated cholesterol, e.g. 26-hydroxycholesterol, or a pharmaceutically effective derivative thereof e.g. an ester or ether. The invention is further directed to a method of treating a patient suffering from said skin disease comprising applying to the effected skin said therapeutic composition. The invention is also directed to the topical application of these compositions to the skin to decrease inflammation.
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(2008/06/13)
SIMPLE METHODS FOR THE N-ALKYLATION OF LACTAMS
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Kramarova, E. P.,Shipov, A. G.,Orlova, N. A.,Artamkina, O. B.,Belavin, I. Yu.,Baukov, Yu. I.
p. 970 - 979
(2007/10/02)
Central nervous system active compounds. I. The synthesis of some caprolactam derivatives substituted at N1, C2 and C3
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Duong,Prager,Ward,Kerr
p. 2651 - 2665
(2007/10/04)
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