title: Synthesis and in-vitro evaluation of 2-amino-4-arylthiazole as inhibitor of 3D polymerase against foot-and-mouth disease (FMD).
abstract: 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.
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Kwi-Wan
authors: KW
authors: Jeong
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Jung-Hun
authors: JH
authors: Lee
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Sun-Mi
authors: SM
authors: Park
authors: 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.
authors: Joo-Hyung
authors: JH
authors: Choi
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Dae-Youn
authors: DY
authors: Jeong
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Dong-Hwa
authors: DH
authors: Choi
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea.
authors: Yeonju
authors: Y
authors: Nam
authors: 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.
authors: Jong-Hyeon
authors: JH
authors: Park
authors: 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.
authors: Kwang-Nyeong
authors: KN
authors: Lee
authors: 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. Electronic address: beliefsk@korea.kr.
authors: Su-Mi
authors: SM
authors: Kim
authors: Bio-Center, Gyeonggi Institute of Science and Technology Promotion, 147 Gwanggyo-ro, Yongtong-gu, Suwon-si, Gyeonggi-do, Republic of Korea. Electronic address: medichem@gstep.re.kr.
authors: Jin-Mo
authors: JM
authors: Ku
mesh_terms: D000818:Animals; D000956:Antigens, Viral / Q000378:metabolism; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005536:Foot-and-Mouth Disease / Q000188:drug therapy* / Q000378:metabolism; D029544:Foot-and-Mouth Disease Virus / Q000187:drug effects* / Q000201:enzymology; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013552:Swine; D017361:Viral Nonstructural Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000956:Antigens, Viral; D000998:Antiviral Agents; D004791:Enzyme Inhibitors; D017361:Viral Nonstructural Proteins; C103557:virus-infection-associated antigen, Foot-and-mouth disease virus
keywords: 2-Amino-4-arylthiazole; 3D polymerase (3Dpol); Antiviral; Foot-and-mouth disease virus (FMDV); Inhibitor