Synthesis and anorectic activity of 2H-4,6-dimethyl-2-[(4- phenylpiperazin-1-yl)methyl]-3-oxo-2,3-dihydroisothiazolo[5,4-b]pyridin e.

The synthesis of 2H-4,6-dimethyl-2-[(4- phenylpiperazin-1-yl)methyl]-3-oxo-2,3-dihydroisothiazolo[5, 4-b]pyridine. (3) and its biological properties are described. Compound 3 pharmacologically evaluated in vivo by use of behavioral tests showed to have a profile of activity characteristic of stimulation of the central serotoninergic system, mostly 5-HT52A receptors (anorectic action: 2 mg/kg i.p., 8.5 mg/kg po) However, receptor activity of isothiazolopyridine 3 was not confirmed in vitro using 5-HT2A and 5-HT1A receptor binding technique. Molecular modeling studies demonstrated that it is difficult to predict bioactive conformation of title molecule 3.