Structure Activity Relationships of 2-Phenylpyrazolo(4,3-c)quinolin-3-ones and Their N-and O-Methyl Analogues at BenzodiazepineReceptors. -The structure activity relationship of the parent compounds (I), which are high affinity ligands at central benzodiazepine receptors (BZR), cannot be determined unambiguously due to the potential of tautomerism. Thus, methylated derivatives (II) and (III) are synthesized to find out the biologically active tautomers. (IIa) and (IIb) show relatively high affinities for BZR, compared to (IIc) and (III), but less than (I) . The presence of a proton donor in (I) does not appear to substantially contribute to agonist activity of (Ib), but may be essential for the inverse agonist property of (Ia).-(FRYER, R. I.; RIOS, R.; ZHANG, P.; GU, Z.-Q.; WONG, G.; BASILE, A. S.; SKOLNICK, P.; Med. Chem. Res. 3 (1993) 2, 122-130; Dep. Chem., Rutgers, State Univ. N. J., Newark, NJ 07102, USA; EN)
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