A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT 1A receptor ligands

G Caliendo, F Fiorino, E Perissutti, B Severino…

Index: Caliendo, Giuseppe; Fiorino, Ferdinando; Perissutti, Elisa; Severino, Beatrice; Scolaro, Daniela; Gessi, Stefania; Cattabriga, Elena; Borea, Pier Andrea; Santagada, Vincenzo European Journal of Pharmaceutical Sciences, 2002 , vol. 16, # 1-2 p. 15 - 28

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Citation Number: 40

Abstract

A series of novel 1, 2, 3-4-benzoyltriazole and saccharine derivatives were designed and synthesized by microwave heating. They were evaluated on a battery of receptors, including serotonin 5-HT1A, 5-HT2A and 5-HT2C, and the most interesting compounds were further evaluated on dopaminergic D1, D2 and adrenergic α1, α2 receptors. Conventional and microwave heating of the reactions were compared. Synthesis by microwave heating gave ...