II. Preparación de nuevas fenilamidas anticonvulsionantes

作者: Guillermo Carvajal-Sandoval , Sergio Enrique Meza-Toledo

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摘要: En el presente trabajo se prepararon una serie nueva de fenilamidas anticonvulsionantes conteniendo los grupos trifluorometilo, fluor, bromo y cloro en anillo aromatico compuestos DL-2- hidroxi-2-etil-2-fenil acetamida (DL-HEPA), DL-3-hidroxi-3-etil- 3-fenilpropionamida (DL-HEPP) DL-4-hidroxi-4-etil-4-fenilbutiramida (DL-HEPB). Los preparados presentaron actividad anticonvulsionante bastante significativa contra las convulsiones la muerte provocadas por metrazol ratones. La incorporacion halogenos DL-HEPA, DL-HEPP DL-HEPB condujo a con similar del fenobarbital. Se presentan evidencias que preparadas podrian actuar como antagonistas receptores GABA.

参考文章(27)
Mary Chebib, Jane R. Hanrahan, Kenneth N. Mewett, Rujee K. Duke, Graham A.R. Johnston, Ionotropic GABA Receptors as Therapeutic Targets for Memory and Sleep Disorders Annual Reports in Medicinal Chemistry. ,vol. 39, pp. 13- 23 ,(2004) , 10.1016/S0065-7743(04)39002-0
Rd. Khling, NEUROSCIENCE: GABA Becomes Exciting Science. ,vol. 298, pp. 1350- 1351 ,(2002) , 10.1126/SCIENCE.1079446
Sonia Arbilla, Linda Kamal, Salomon Z. Langer, Presynaptic GABA autoreceptors on gabaergic nerve endings of the rat substantia nigra European Journal of Pharmacology. ,vol. 57, pp. 211- 217 ,(1979) , 10.1016/0014-2999(79)90367-4
Ricardo Tapia, René Raúl Drucker-Colín, Graciela Meza-Ruíz, Lilia Durán, Giulio Levi, Neurophysiological and Neurochemical Studies on the Action of the Anticonvulsant γ-Hydroxy, γ-Ethyl, γ-Phenyl-Butyramide Epilepsia. ,vol. 20, pp. 135- 145 ,(1979) , 10.1111/J.1528-1157.1979.TB04786.X
N. Bowery, GABAbeta Receptor Pharmacology Annual Review of Pharmacology and Toxicology. ,vol. 33, pp. 109- 147 ,(1993) , 10.1146/ANNUREV.PHARMTOX.33.1.109
Simon Brailowsky, Teresa Montiel, Elizabeth Hernández, Christian Marescaux, Marguerite Vergnes, Effects of 3-hydroxy,3-ethyl,3-phenylpropionamide (HEPP) on rat models of generalized and focal epilepsy. Epilepsy Research. ,vol. 11, pp. 167- 172 ,(1992) , 10.1016/0920-1211(92)90095-B
Z. Liu, M. Vergnes, A. Depaulis, C. Marescaux, Involvement of intrathalamic GABAB neurotransmission in the control of absence seizures in the rat. Neuroscience. ,vol. 48, pp. 87- 93 ,(1992) , 10.1016/0306-4522(92)90340-8
Atsuo Fukuda, Diuretic soothes seizures in newborns. Nature Medicine. ,vol. 11, pp. 1153- 1154 ,(2005) , 10.1038/NM1105-1153
P. Gloor, R.G. Fariello, Generalized epilepsy: some of its cellular mechanisms differ from those of focal epilepsy Trends in Neurosciences. ,vol. 11, pp. 63- 68 ,(1988) , 10.1016/0166-2236(88)90166-X