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Advances in Drug Design Based on the Amino Acid Approach: Taurine Analogues for the Treatment of CNS Diseases

Lapdesf-Laboratory of Drug Design, School of Pharmaceutical Sciences, University of São Paulo State (UNESP), Rodovia Araraquara-Jaú Km1, CEP 14.801-902, Araraquara, SP, Brazil
Author to whom correspondence should be addressed.
Pharmaceuticals 2012, 5(10), 1128-1146;
Received: 31 July 2012 / Revised: 24 September 2012 / Accepted: 15 October 2012 / Published: 23 October 2012
(This article belongs to the Special Issue Advances in Drug Design)
Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer’s, Parkinson’s, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment. View Full-Text
Keywords: amino acid; CNS; taurine; analogs amino acid; CNS; taurine; analogs
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Chung, M.C.; Malatesta, P.; Bosquesi, P.L.; Yamasaki, P.R.; Santos, J.L.; Vizioli, E.O. Advances in Drug Design Based on the Amino Acid Approach: Taurine Analogues for the Treatment of CNS Diseases. Pharmaceuticals 2012, 5, 1128-1146.

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