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- Title
Tricyclic Pyridine Derivatives with High Affinity to the Central Benzodiazepine Receptor.
- Authors
Fischer, Ulf; Möhler, Hanns; Schneider, Fernand; Widmer, Ulrich
- Abstract
Novel tricyclic heterocycles were prepared and evaluated for their affinity to the central benzodiazepine receptor. The most potent compounds with IC50's in the nanomolar range were; found among thienoquinolizines and benzo[ a]quinolizines ( cf. Tables 2-5). The central ring of the tricyclic ring system may be partially unsaturated ( cf. Tables 2 and 4) or fully unsaturated ( cf. Tables 3 and 5) without loss of the high affinity to the receptor. The position of the ester group in the pyridinone ring is crucial for good binding ( cf. Tables 1 and 2). It may be replaced by a broad variety of functional groups, e.g. amides, alkyl carbamates, alkyl groups, and hydroxyalkyl groups ( cf. Tables 2-5). In the benzo[ a]quinolizines, shifting the halogen atom from C(10) to C(9) leads to complete loss of affinity to the benzodiazepine receptor ( cf. Table 4).
- Publication
Helvetica Chimica Acta, 1990, Vol 73, Issue 4, p763
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/hlca.19900730402