The synthesis of new 3-alkyloxycarbonyl-, 3-cyclo-alkyloxycarbonyl-, 3- aryloxycarbonyl derivatives of pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their binding affinities at the central benzodiazepine receptor (BZR) are reported. The 3-propynyl ester 10 and the 3-benzyl ester 16, having the best affinity values, were chosen for in vivo testing.
BENZODIAZEPINE RECEPTOR (BZR) LIGANDS.5. NEW 3-ALKYLOXYCARBONYL-, 3-CYCLOALKYLOXYCARBONYL-,3-ARYLOXYCARBONYLDERIVATIVES OF PYRAZOLO [5,1-C][1,2,4]BENZOTRIAZINE 5-OXIDES: A STUDY ON THE 3-ESTER FUNCTION MODIFICATION / A. COSTANZO, G. GUERRINI, G. CICIANI, F. BRUNI, S. SELLERI, B. COSTA, C. MARTINI, P. MALMBERG, A. IPPONI, A. LUCACCHINI. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - STAMPA. - 9:(1999), pp. 322-339.
BENZODIAZEPINE RECEPTOR (BZR) LIGANDS.5. NEW 3-ALKYLOXYCARBONYL-, 3-CYCLOALKYLOXYCARBONYL-,3-ARYLOXYCARBONYLDERIVATIVES OF PYRAZOLO [5,1-C][1,2,4]BENZOTRIAZINE 5-OXIDES: A STUDY ON THE 3-ESTER FUNCTION MODIFICATION
COSTANZO, ANNARELLA;GUERRINI, GABRIELLA;CICIANI, GIOVANNA;BRUNI, FABRIZIO;SELLERI, SILVIA;MALMBERG, PETRA;
1999
Abstract
The synthesis of new 3-alkyloxycarbonyl-, 3-cyclo-alkyloxycarbonyl-, 3- aryloxycarbonyl derivatives of pyrazolo[5,1-c][1,2,4]benzotriazine 5-oxides and their binding affinities at the central benzodiazepine receptor (BZR) are reported. The 3-propynyl ester 10 and the 3-benzyl ester 16, having the best affinity values, were chosen for in vivo testing.
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