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

By G. CALIENDO, F. FIORINO, E. PERISSUTTI, B. SEVERINO, D. SCOLARO, GESSI S., E. CATTABRIGA, P.A. BOREA and V. SANTAGADA

Abstract

A series of novel 1,2,3-4-benzoyltriazole and saccharine derivatives were designed and synthesized by microwave heating. They were\ud evaluated on a battery of receptors, including serotonin 5-HT 5-HT and 5-HT , and the most interesting compounds were further 1A, 2A 2C\ud evaluated on dopaminergic D , D and adrenergic a , a receptors. Conventional and microwave heating of the reactions were compared. 1 2 1 2\ud Synthesis by microwave heating gave the desired compounds in better yields than those obtained by conventional heating. The overall\ud times for the syntheses were considerably reduced. All compounds displayed moderate affinity for 5-HT receptor. The most interesting 1A\ud compound 33 showed a high affinity (K 593 nM) which was combined with no affinity on the other receptors considered

Year: 2002
OAI identifier: oai:iris.unife.it:11392/1204014
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