104604-15-1Relevant articles and documents
78. Tricyclic pyridine derivatives with high affinity to the central benzodiazepine receptor
Fischer,Mohler,Schneider,Widmer
, p. 763 - 781 (2007/10/02)
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).
Tricyclic pyridine derivatives and pharmaceutical compositions
-
, (2008/06/13)
Compounds of the formula STR1 or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described. The compounds of formula I possess pronounced muscle relaxant, sedative-hypnotic, anticonvulsive and anxiolytic properties and have low toxicity.
