CNS-active agents

Another CNS active agent in this structural class is the tranquilizer-antidepressant caroxazone (52). Its published synthesis begins by reductive aminatiwi of salicylaldehyde and glycinamide to give The synthesis is completed by reaction with phosgene and sodium bicarbonate. ... 

These are the exact rings. They are easy to make they add a sense of sophistication to an otherwise pedestrian scientific paper and they often represent the inactive extremes in a receptor site study of a structure activity relationship study of a CNS-active agent. But the compounds represented here appear to have simply the wrong properties, somehow, and should not really be seriously considered in the quest for understanding of the remarkable actions of most of the psychedelic phenethylamines and tryptamines. 

Changes in drug effects are often delayed in relation to changes in plasma concentration. This delay may reflect the time required for the drug to distribute from plasma to the site of action. This will be the case for almost all drugs. The delay due to distribution is a pharmacokinetic phenomenon that can account for delays of a few minutes. This distributional delay can account for the lag of effects after rapid intravenous injection of central nervous system (CNS)-active agents such as thiopental. 

Quinolizidinones can also serve as substrates for Robinson annelation procedures. For example, benzo[c]quinolizidinedione derivative (160) was activated in the position a to the ketone group in C-6 by formylation and then treated with methyl vinyl ketone to yield the pyrido[l,2-/]phenan-thridine (161), which was then functionalized to the CNS active agent (162) <83EUP90526> (Scheme 24). 

Furancarbonamides 248 give good yields of cycloadducts with benzyne. Reduction and flash vacuum pyrolysis of 249 led to isobenzofurans, which were again subjected to benzyne cycloaddition to form 250, of potential interest as CNS-active agents. 

Clement JA, Yoder BJ, Kingston DGI. Natural products as a source of CNS-active agents. Mini-Rev Org Chem 2004 1 183-208. 

German Commission E advises against use during pregnancy or lactation or with concomitant use of other CNS active agents. 

Cyano-2-fluoropyridines are an important class of biologically active compounds that include potent kinase inhibitors, potassium channel inhibitors, and CNS active agents 51-53 (Fig. 1) [51-55]. In addition, fluorinated pyridines can be potentially used as labeling agents for various spectroscopic techniques such as positron emission tomography, X-ray photoelectron spectroscopy, and NMR spectroscopy. 

BunneUe WH, Barlocoo CD, Daanen JF, Dart MJ, Meyer MD, Ryther KB, Schrimpf MR, Sippy KB, Toupence RB (2007) DiazabicycUc CNS active agents. Patent US7265115 (B2), 4 Sept 2007... 

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