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Ring closure reactionsO 0130 DOI: 10.1002/chin.201039042

Tricyclic Dihydroquinazolinones as Novel 5-HT2C Selective and Orally Efficacious anti-Obesity Agents. — Synthesis and biological evaluation of a series of novel and highly selective dihydroquinazolinone-derived 5-HT2C agonists with no detectable agonism of the 5-HT2B receptor are described. Among these, compounds ((+)-II) and ((+)-VI) are identified as agonists which exhibit weight loss in a rat model upon oral dosing. In all cases the racemic final products are resolved by chiral chromatography affording enantiomerically pure substances which are both tested for biological activi-ty. — (AHMAD*, S.; et al.; Bioorg. Med. Chem. Lett. 20 (2010) 3, 1128-1133, DOI:10.1016/j.bmcl.2009.12.014 ; Res. Dev., Bristol-Myers Squibb Co., Princeton, NJ 08543, USA; Eng.) — H. Haber

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