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The synthesis of new barbiturate esters derivatives as intravenous anesthetics: a new dimension of anesthesia route part-IV


Conventional 1-methyl-2-oxybarbiturates and 1-methyl-2-thiobarbiturates are employed as anesthetics and tend to accumulate in the body due to their slow rate of metabolism. As a result, the use of these compounds is restricted to either being an induction agent for anesthesia, subsequently maintained by volatile anesthetics, or for short surgical procedures only. To overcome these limitations of barbiturates as general anesthetics, and to avoid the use of volatile agents, structural modifications of barbiturates molecules as intravenous anesthetics were attempted. It was conceived that, by incorporating metabolically labile ester functions in one or both of the side chain of the barbiturates ring system, this could be achieved. Since this procedure could diminish the likelihood of barbiturates to be accumulated in the body, it would make it possible to get safer barbiturate intravenous anesthetics. This classification arose from the observation that while the biological properties of some drugs are extremely sensitive to minor changes in the stereo-chemical feature, electron distribution, and substituent, there are many other drugs which exhibit similar patterns of biological behavior, despite a wide diversity in their chemical configurations. This has appeared to be the case with the barbiturate esters as discussed.


barbiturates, intravenous anesthetics, metabolically labile ester