Design, synthesis, and evaluation of analogues of 3, 3, 3-trifluoro-2-hydroxy-2-phenyl-propionamide as orally available general anesthetics

I Choudhury-Mukherjee, HA Schenck…

Index: Choudhury-Mukherjee, Indrani; Schenck, Hilary A.; Cechova, Sylvia; Pajewski, Thomas N.; Kapur, Jaideep; Ellena, Jeffrey; Cafiso, David S.; Brown, Milton L. Journal of Medicinal Chemistry, 2003 , vol. 46, # 12 p. 2494 - 2501

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Citation Number: 24

Abstract

We have recently discovered a novel class of compounds that have oral general anesthetic activity, potent anticonvulsant activity, and minimal hemodynamic effects. The 3, 3, 3-trifluoro- 2-hydroxy-2-phenyl-propionamide (1) demonstrated potent ability to reduce the minimum alveolar concentration (MAC) of isoflurane, with no effects on heart rate or blood pressure at therapeutic concentrations. Analogue 1 also had potent oral anticonvulsant activity ...