70520-59-1Relevant academic research and scientific papers
A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT1A receptor ligands
Caliendo, Giuseppe,Fiorino, Ferdinando,Perissutti, Elisa,Severino, Beatrice,Scolaro, Daniela,Gessi, Stefania,Cattabriga, Elena,Borea, Pier Andrea,Santagada, Vincenzo
, p. 15 - 28 (2007/10/03)
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 the desired compounds in better yields than those obtained by conventional heating. The overall times for the syntheses were considerably reduced. All compounds displayed moderate affinity for 5-HT1A receptor. The most interesting compound 33 showed a high affinity (Ki=93 nM) which was combined with no affinity on the other receptors considered.
UNSATURATED CARBONYL-CONTAINING COMPOUNDS. XXVIII. CYCLOADDITION OF ORGANIC AZIDES TO α-ACETYLENIC KETONES AND ACIDS
Vereshchagin, L. I.,Tikhonova, L. G.,Maksikova, A. V.,Serebryakova, E. S.,Proidakov, A. G.,Filippova, T. M.
, p. 641 - 648 (2007/10/02)
The reaction of α-acetylenic ketones and acids with organic azides leads to the formation of 1-alkyl(aryl)-4-acyl(carboxy)-1,2,3-triazoles or to a mixture of the 1,4- and 1,5-disubstituted isomers.The effect of the structure of the initial compound and of the solvent on the direction of cycloaddition was investigated.
