A Selective 5-ht Reuptake Inhibitor Design And Synthesis Of Two Blood Products, Virus Inactivation Agent

Depressive illness which placed the significant public health and economic problems upon society was chiefly believed to be associated with the deficiency of 5-Hydroxy tryptamine(5-HT). Tricyclic antidepressants(TCAs) known to inhibit the presynaptic uptake of norepinephrine(NE) and 5-HT were plagued by antichololinergic and cardiovascular side effect, while seritonin-selective reuptake inhibitors(SSRIs) proved to be more selective in their pharmacology burded with fewer side effect. Thus, the development of new and more effective SSRIs to separate the antidepressant properties from the side effects is a subject of continuing interest.In order to search for new selective inhibitors of the 5-HT, the computer-aided drug design (CADD) technology was applied.By using the comparative molecular field analysis(CoMFA), a 3D-QSAR model was established to display the relationship between structure and the potency for inhibition of 5-HT uptake. Also another pharmacophore model was made revealing the relationship between structure and selectivity relative to inhibition of the serotonin transporter(5-HTT) and norepinephrine transporter(NET).Based on the conformation analysis and pharmacophore information of SSRIs, flexible database searching from the NCI-3D and Maybridge-3D database was performed. Eighteen classes of promising compounds were identified. The structures of the compound showed new scaffolds for the design of SSRIs.Fifty noval target compounds have been synthesized. Activity assays are in test.Concerns over the safety of the blood supply have spurred the exploration of viral inactivation strategy for the treatment of...