Jeong Kwi-Wan, Lee Jung-Hun, Park Sun-Mi, Choi Joo-Hyung, Jeong Dae-Youn, Choi Dong-Hwa, Nam Yeonju, Park Jong-Hyeon, Lee Kwang-Nyeong, Kim Su-Mi, Ku Jin-Mo
Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
Foot-and-Mouth Disease Division, Animal and Plant Quarantine Agency, Ministry of Agriculture, Food and Rural Affairs, 175 Anyangro, Manan-gu, Anyang-si, Gyeonggi-do, Republic of Korea.
Eur J Med Chem. 2015 Sep 18;102:387-97. doi: 10.1016/j.ejmech.2015.08.020. Epub 2015 Aug 12.
Foot-and-mouth disease (FMD) is a highly contagious vesicular disease of livestock caused by a highly variable RNA virus, foot-and-mouth disease virus (FMDV). One of the targets to suppress expansion of and to control FMD is 3D polymerase (FMDV 3Dpol). In this study, 2-amino-4-arylthiazole derivatives were synthesized and evaluated for their inhibitory activity against FMDV 3Dpol. Among them, compound 20i exhibited the most potent functional inhibition (IC50 = 0.39 μM) of FMDV 3D polymerase and compound 24a (EC50 = 13.09 μM) showed more potent antiviral activity than ribavirin (EC50 = 1367 μM) and T1105 (EC50 = 347 μM) with IBRS-2 cells infected by the FMDV O/SKR/2010 strain.
口蹄疫(FMD)是一种由高度可变的RNA病毒——口蹄疫病毒(FMDV)引起的家畜高度传染性水疱病。抑制口蹄疫传播和控制口蹄疫的目标之一是3D聚合酶(FMDV 3Dpol)。在本研究中,合成了2-氨基-4-芳基噻唑衍生物,并评估了它们对口蹄疫病毒3Dpol的抑制活性。其中,化合物20i表现出对FMDV 3D聚合酶最有效的功能抑制(IC50 = 0.39 μM),化合物24a(EC50 = 13.09 μM)在感染FMDV O/SKR/2010毒株的IBRS-2细胞中显示出比利巴韦林(EC50 = 1367 μM)和T1105(EC50 = 347 μM)更强的抗病毒活性。