Title of article :
Synthesis of 3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, displaying combined 5-HT uptake inhibiting and α2-adrenoceptor antagonistic activities. Part 2: Further exploration on the cinnamyl moiety
Author/Authors :
Joaqu??n Pastor، نويسنده , , Jes?s Alc?zar، نويسنده , , Rosa M. Alvarez، نويسنده , , J. Ignacio Andrés، نويسنده , , José M. Cid، نويسنده , , Ana I. De Lucas، نويسنده , , Adolfo D??az، نويسنده , , Javier Fernandez-Suarez، نويسنده , , Luis M. Font، نويسنده , , Laura Iturrino، نويسنده , , Celia Lafuente، نويسنده , , Sonia Mart??nez، نويسنده , , Margot H. Bakker، نويسنده , , Ilse Biesmans، نويسنده , , Lieve I. Heylen، نويسنده , , Anton A. Megens، نويسنده ,
Abstract :
In our previous paper we have described the synthesis of a series of 3-piperazinylmethyl-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazoles, as novel dual 5-HT reuptake inhibitors and α2-adrenoceptor antagonists. That investigation led to the identification of the cinnamyl fragment as the most suitable moiety for combined activity. This paper outlines a further optimisation programme, focused on the exploration of the aromatic ring present on the cinnamyl moiety of compounds 1, 2 and 3.
Keywords :
a2 Antagonists.q For Part 1 , see Ref. 4. , 5-HT reuptake inhibitors , Isoxazolines