121st General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Event Hall
Time 4월 19일 (목요일) 11:00~12:30
Code MEDI.P-645
Subject Discovery of Highly Potent Inhibitors against Rhinovirus Replication
Authors Prashant Chakrasali, SOO BONG HAN1, Young-Sik Jung1,*
Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, University of Science & Technology, Korea
1Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Korea
Abstract Human Rhinoviruses (hRVs) are major pathogens for both upper and lower respiratory tract. These infections are serious threat to patients with asthma, chronic obstructive pulmonary disorder (COPD), or cystic fibrosis in whom respiratory tract infections with RVs can lead to exacerbations. Phosphatidylinositol 4-kinase IIIβ (PI4KB) is indispensable for the replication of various positive-sense single stranded RNA viruses, which hijack this cellular enzyme to remodel intracellular membranes (ER) of infected cells to set up the functional replication machinery. Therefore, the inhibition of this PI4K isoforms leads to the arrest of viral replication. Here in we report on the synthesis of PI4KIIIB inhibitors, through combination of high throughput screening (HTS) and known PI4K inhibitors. Synthesized compounds shows 2 digit nanomolar anti hRV activity with high selective indices.
E-mail prashant@krict.re.kr