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2005
Pyrazole derivatives
R 0180
Synthesis, Central and Peripheral Benzodiazepine Receptor Affinity of Pyrazole
Pyrazole-Containing Polycyclic Derivatives. — The new pyrazole-condensed
12- 127 and
6,5,5 tricyclic compounds (III), (IV), (VII), and (IX) are synthesized and their binding
affinity at both central (CBR) and peripheral (PBR) benzodiazepine receptors is measured. In addition, some 1-aryl-5-phenylpyrazole derivatives are prepared and tested
for comparison with their corresponding rigid tricyclic analogues. Indenopyrazole
(IVb) emerges as a new potent and selective CBR ligand while diethylamide (VIIa) is
identified as a less potent but highly selective PBR ligand. — (CAMPAGNA*, F.;
PALLUOTTO, F.; CAROTTI, A.; MACIOCCO, E.; Farmaco 59 (2004) 11, 849-856;
Dip. Farmacochim., Univ. Bari, I-70125 Bari, Italy; Eng.) — H. Hoennerscheid
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