title: Identification of a series of 1,3,4-trisubstituted pyrazoles as novel hepatitis C virus entry inhibitors.
abstract: In this report we describe the identification of novel pyrazole analogs as potent hepatitis C virus (HCV) entry inhibitor. The pyrazoles were identified by our phenotypic high-throughput screening using infectious HCV. A series of pyrazole derivatives was synthesized and evaluated for inhibitory activity against HCV in the infectious cell culture system. Through evaluation of selected compounds we observed that the pyrazoles did not interfere with HCV RNA replication but with viral entry as shown by experiments with HCV replicons and HCV pseudo particles, respectively.
authors.affiliation: Medicinal Chemistry Group, Institut Pasteur Korea (IP-K), Sampyeong-dong 696, Bundang-gu, Seongnam-si, Gyeonggi-do 463-400, Republic of Korea.
authors.forename: Jong Yeon
authors.initials: JY
authors.lastname: Hwang
authors.forename: Hee-Young
authors.initials: HY
authors.lastname: Kim
authors.forename: Dong-Sik
authors.initials: DS
authors.lastname: Park
authors.forename: Jihyun
authors.initials: J
authors.lastname: Choi
authors.forename: Sung Min
authors.initials: SM
authors.lastname: Baek
authors.forename: Keumhyun
authors.initials: K
authors.lastname: Kim
authors.forename: Soohyun
authors.initials: S
authors.lastname: Kim
authors.forename: Sikwang
authors.initials: S
authors.lastname: Seong
authors.forename: Inhee
authors.initials: I
authors.lastname: Choi
authors.forename: Hong-gun
authors.initials: HG
authors.lastname: Lee
authors.forename: Marc Peter
authors.initials: MP
authors.lastname: Windisch
authors.forename: Jinhwa
authors.initials: J
authors.lastname: Lee
mesh_terms: D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D016174:Hepacivirus / Q000187:drug effects* / Q000502:physiology; D006526:Hepatitis C / Q000188:drug therapy* / Q000235:genetics; D006801:Humans; D011720:Pyrazoles / Q000737:chemistry / Q000494:pharmacology*; D053586:Virus Internalization / Q000187:drug effects
chemical_list: D000998:Antiviral Agents; D011720:Pyrazoles
keywords: Entry inhibitor; Hepatitis C virus; Infectious cell culture system; Phenotypic high-throughput screening; Pyrazole