作为研究计划的一部分,制备了咪唑并[1,5-g] [1,4]二氮杂derivatives衍生物7a和7b,它们是没有芳香环的TIBO类似物,目的是寻找对HIV-2具有抗病毒活性和抗药性的菌株。 HIV-1。N-三苯甲基和N-甲苯磺酰基4-(2-氯乙基)-咪唑与适当的氨基醇的缩合得到化合物10a-c和16a-e。这些中间体中的羟基通过转化为相应的氯衍生物或通过甲苯磺酰基的N→O转移而被激活,从而使[1,4]二氮杂卓环闭合。然而,仅环化至化合物13a和13b被证明是有效的。这些产物被转化为目标分子7通过它们的C-2阴离子与S 8反应。化合物7a,b和13a,b在细胞培养物中的体外评估(CEM SS / HIV-1-LAI和CEM SS / HIV 1 nevirapine抗性细胞)显示只有13b表现出最小的活性。
The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
[EN] SMALL-MOLECULE AGENTS WITH ANTIVIRAL ACTIVITY AGAINST RNA VIRUSES<br/>[FR] AGENTS À PETITES MOLÉCULES AYANT UNE ACTIVITÉ ANTIVIRALE CONTRE DES VIRUS À ARN
申请人:[en]FUNDACIÓN UNIVERSIDAD CATÓLICA DE VALENCIA SAN VICENTE MÁRTIR
公开号:WO2022175384A1
公开(公告)日:2022-08-25
The present invention relates to the use of small organic compounds, or a salt or solvate thereof, for the treatment and/or prevention of viral infections by RNA-viruses, preferably from the familyCoronaviridae, Orthomyxoviridae, Filoviridae, Flaviviridae, Retroviridae and Togaviridae, such as SARS-CoV-2.