Τίτλος:
Novel compounds designed as antistress agents
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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) or3,5-di-tert-butyl-4-hydroxybenzoic acid (6). Compounds 5 and 6 inhibited lipid peroxidation, IC50 1.1 and 24 μM. 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%. ©2009 American Chemical Society.
Συγγραφείς:
Tsiakitzis, K.C.
Rekka, E.A.
Kourounakis, A.P.
Kourounakis, P.N.
Περιοδικό:
Journal of Medicinal Chemistry
Λέξεις-κλειδιά:
4 aminobutyric acid derivative; 7 chloro 5 (2 chlorophenyl) 1,3 dihydro 2 oxo 2h 1,4 benzodiazepin 3 yl 4 (3,5 di tert butyl 4 hydroxybenzoylamino)butanoate; 7 chloro 5 (2 chlorophenyl) 1,3 dihydro 2 oxo 2h 1,4 benzodiazepin 3 yl 4 (6 hydroxy 2,5,7,8 tetramethylchroman 2 carbonylamino)butanoate; antioxidant; aspartic proteinase; cytochrome P450; erythromycin; lorazepam; radical; trolox C; unclassified drug; uropepsinogen, amidation; animal experiment; animal model; article; controlled study; demethylation; drug metabolism; drug screening; drug synthesis; esterification; hyperlipidemia; lipid peroxidation; nonhuman; oxidative stress; rat; stress, Amides; Animals; Anti-Anxiety Agents; Antioxidants; Benzoic Acids; Brain; Carboxylic Acids; Chromans; Drug Design; Dyslipidemias; Esterification; gamma-Aminobutyric Acid; Lipid Peroxidation; Lorazepam; Male; Oxidative Stress; Rats; Stress, Physiological
