首页> 外国专利> USE OF THE ACETIC ACID COMPOUND 2-1-(1R)-1-3-2-(7-CHLOROQUIN OLIN-2-YL) ETENYL PHENYL-3-2-(2-HYDROXYPROPAN-2-) PHENYL PROPYL SULFANYLMETHYL CYCLOPROPYL AS ALOSTERIC INHIBITOR OF THE DENGUE VIRUS NS2B/NS3 PROTEASE.

USE OF THE ACETIC ACID COMPOUND 2-1-(1R)-1-3-2-(7-CHLOROQUIN OLIN-2-YL) ETENYL PHENYL-3-2-(2-HYDROXYPROPAN-2-) PHENYL PROPYL SULFANYLMETHYL CYCLOPROPYL AS ALOSTERIC INHIBITOR OF THE DENGUE VIRUS NS2B/NS3 PROTEASE.

机译:乙酸化合物2- [1-[[((1R)-1- [3- [2-(7-氯喹OLIN-2-YL)ETENYL]] PHENYL] -3- [2-(2-HYDROXYPROPAN- 2-)作为登革热病毒NS2B / NS3蛋白酶的芳香族抑制剂,[苯基] [丙基] [亚磺基] [环丙基]。

摘要

The present disclosure is related to a new use of the acetic acid compound 2-[1-[[(1R)-1-[3-[2-(7-chloroquinolin-2-yl) ethenyl] phenyl]-3-[2-(2-hydroxypropan-2-yl) phenyl] propyl] sulfanylmethyl] cyclopropyl] (Montelukast) as an allosteric inhibitor of the the dengue virus protease NS2B / NS3, with the aim of eradicating the reproduction of the dengue virus in infected people by adhesion of the compound to the activation site of the complex forming the NS2B and NS3 proteins, proteases precursors of the dengue viral polyprotein. The compound is effective when the virus has infected human cells, specifically monocytes, hepatocytes, neurons, kidney cells. The compound binds to a conserved site behind the active site, causing the NS2B and NS3 protein complex to lose the protease function. The acetic acid compound 2-[1-[[(1R)-1-[3-[2-(7-chloroquinolin-2-yl) ethenyl] phenyl]-3-[2-(2-hydroxypropan-2-yl) phenyl] propyl] sulfanylmethyl] cyclopropyl] (Montelukast) is characterized by having a m inimal inhibitory dose of 160 ug/ml and a maximum inhibitory dose of 10 mg/ml in humans.
机译:本公开内容涉及乙酸化合物2- [1-[[((1R)-1-] [3- [2-(7-氯喹啉-2-基)乙烯基]苯基] -3- [的新用途。 2-(2-羟基丙-2-基)苯基]丙基]硫烷基甲基]环丙基](孟鲁司特)作为登革热病毒蛋白酶NS2B / NS3的变构抑制剂,目的是消除登革热病毒在感染人群中的繁殖。通过将化合物粘附到形成NS2B和NS3蛋白的复合物的激活位点上,这是登革热病毒多蛋白的蛋白酶前体。当病毒感染人细胞,特别是单核细胞,肝细胞,神经元,肾细胞时,该化合物有效。该化合物与活性位点后面的保守位点结合,导致NS2B和NS3蛋白复合物失去蛋白酶功能。乙酸化合物2- [1-[[((1R)-1- [3- [2-(7-氯喹啉-2-基)乙烯基]苯基] -3- [2-(2-羟基丙-2-基(Montelukast)的特征在于在人中的最小抑菌剂量为160 ug / ml,最大抑菌剂量为10 mg / ml。

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