| Title | Novel Compounds Designed as Antistress Agents. | | Author(s) | Tsiakitzis KC, Rekka EA, Kourounakis AP, Kourounakis PN | | Institution | Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 54124 Thessaloniki, Greece. | | Source | J Med Chem 2009 Oct 28. | | Abstract | Agents against biologic stress were designed, containing GABA esterified with lorazepam and amidated with (R)-6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid (5) or 3,5-di-tert-butyl-4-hydroxybenzoic acid (6). Compounds 5 and 6 inhibited lipid peroxidation, IC(50) 1.1 and 24 muM. Oxidative damage accompanied stress, 5 and 6 reduced radical attack, uropepsinogen, and morphological changes. Stress increased drug metabolism. Treatment with 5 reduced cytochrome P450 and N-demethylation of erythromycin, 35 and 40%. Compounds 5 and 6 decreased lipidemic indices of hyperlipidemic rats 40-63%. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 19863055 |
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