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2005
Pyrazole derivatives
R 0180
Design, Synthesis and Evaluation of Bicyclic Benzamides as Novel 5-HT1F RecepAgonists. — The indole nucleus, embodied in the original lead structure, is
15- 111 tor
replaced by some bicyclic systems including indoline (II), indazole (IV), "inverted" indazole (XI), and benzisoxazole, providing more potent and selective 5-HT1F receptor
ligands. In addition, the 5-HT1A receptor selectivity of the indoline- and benzisoxazole-based 5-HT1F receptor agonists can be improved by modification of the benzoyl
moiety of the benzamides. The geometries of the bicyclic systems, and not the nature
of hybridization of the linking atom, are responsible for receptor recognition. —
(ZHANG*, D.; et al.; Bioorg. Med. Chem. Lett. 14 (2004) 24, 6011-6016; Lilly Res.
Lab., Lilly Corp. Cent., Eli Lilly Co., Indianapolis, IN 46285, USA; Eng.) —
H. Hoennerscheid
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