DESIGN OF A NOVEL COGNITIVE ENHANCER YDRO-5H,10H-PYRROLO[1,2-A][1,4]DIAZOCIN-5,10-DIONE

Authors
MAZUROV AA ANDRONATI SA KOROTENKO TI SOKOLENKO NI DYADENKO AI SHAPIRO YE GORBATYUK VY VORONINA TA
Citation
Aa. Mazurov et al., DESIGN OF A NOVEL COGNITIVE ENHANCER YDRO-5H,10H-PYRROLO[1,2-A][1,4]DIAZOCIN-5,10-DIONE, Bioorganic & medicinal chemistry letters, 6(21), 1996, pp. 2595-2600
Citations number
30
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
21
Year of publication
1996
Pages
2595 - 2600
Database
ISI
SICI code
0960-894X(1996)6:21<2595:DOANCE>2.0.ZU;2-R
Abstract
A new cognitive enhancer (8S, 10aS)-8-carbamoyl-1,2,3,6,7,8,9,10a-octa hydro-5H, 10H-pyrrolo[1,2-a][1,4]diazocin-5,10-dione (3) has been desi gned based on the approach consisting of two steps: 1) ''obligatory'' replacement of histidine with glutamine in TRH; 2) the application of conformational constraints for putative bioactive conformation of [Gln (2)]-TRH. 3 reversed on 100% electroconvulsive shock-induced amnesia a t doses of 0.1 and 1.0 mg/kg and on 83% scopolamine-induced amnesia at a dose of 1 mg/kg, using passive avoidance test. Copyright (C) 1996 E lsevier Science Ltd