2003
DOI: 10.1002/chin.200308137
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Synthesis and Evaluation of 5‐HT2A and 5‐HT2C Receptor Binding Affinities of Novel Pyrimidine Derivatives.

Abstract: 14 examples) by a simple nucleophilic substitution reaction to find potential anxiolytic or antipsychotic agents with selective 5-HT 2C affinity is reported. Compound (IIId) possesses the highest potency in this series. (No yields given.) -(BOZSING*, D.; SIMONEK, I.; SIMIG, G.; JAKOCZI, I.; GACSALYI, I.; LEVAY, G.; TIHANYI, K.; SCHMIDT, E.; Bioorg. Med. Chem. Lett. 12 (2002) 21, 3097-3099; Chem. Res. Div., EGIS Pharm. Ltd., H-1475 Budapest, Hung.; Eng.) -M. Schroeter 08-137

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“…Therefore, with the aim to obtain selective agents for 5-HT 2C or 5-HT 2A receptor, they prepared a variety of compounds structurally related to 373 (Table 41) [43]. Introduction of a methyl group at the 2-position on the benzyl group linked to the piperazine (compound 374) led to significant increase in 5-HT 2C receptor affinity, whereas the presence of a methyl in 4-position was less tolerated.…”
Section: Piperazine Containing Structurementioning
confidence: 99%
“…Therefore, with the aim to obtain selective agents for 5-HT 2C or 5-HT 2A receptor, they prepared a variety of compounds structurally related to 373 (Table 41) [43]. Introduction of a methyl group at the 2-position on the benzyl group linked to the piperazine (compound 374) led to significant increase in 5-HT 2C receptor affinity, whereas the presence of a methyl in 4-position was less tolerated.…”
Section: Piperazine Containing Structurementioning
confidence: 99%