Discovery and characterization of a novel 7-aminopyrazolo[1,5-a]pyrimidine analog as a potent hepatitis C virus inhibitor

A series of 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) derivatives was screened via phenotypic cell-based assay. Among the compounds tested, compound 32 turned out to be the most promising with 0.28μM EC50 value in the infectious HCVcc. We describe a novel 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) deri...

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Published in:Bioorganic & medicinal chemistry letters 2012-12, Vol.22 (24), p.7297-7301
Main Authors: Hwang, Jong Yeon, Windisch, Marc Peter, Jo, Suyeon, Kim, Keumhyun, Kong, Sunju, Kim, Hyoung Cheul, Kim, Soohyun, Kim, Heeyoung, Lee, Myung Eun, Kim, Youngmi, Choi, Jihyun, Park, Dong-Sik, Park, Eunjung, Kwon, Jeongjin, Nam, Jiyoun, Ahn, Sujin, Cechetto, Jonathan, Kim, Junwon, Liuzzi, Michel, No, Zaesung, Lee, Jinhwa
Format: Article
Language:English
Subjects:
7-Aminopyrazolopyrimidine
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Antiviral Agents - chemistry
Antiviral Agents - metabolism
Antiviral Agents - pharmacology
Biological and medical sciences
Cell culture
Cell Proliferation - drug effects
Dose-Response Relationship, Drug
Drug Discovery
Drug Evaluation, Preclinical
Drug Stability
Hepacivirus - drug effects
Hepatitis C virus
Humans
Infectious cell culture system
Medical sciences
Microbial Sensitivity Tests
Molecular Structure
Pharmacology. Drug treatments
Phenotypic high-throughput screening
Pyrazoles - chemistry
Pyrazoles - metabolism
Pyrazoles - pharmacology
Pyrimidines - chemistry
Pyrimidines - metabolism
Pyrimidines - pharmacology
Rats
Structure-Activity Relationship
Structure-activity relationships
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Summary:A series of 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) derivatives was screened via phenotypic cell-based assay. Among the compounds tested, compound 32 turned out to be the most promising with 0.28μM EC50 value in the infectious HCVcc. We describe a novel 7-aminopyrazolo[1,5-a]pyrimidine (7-APP) derivative as a potent hepatitis C virus (HCV) inhibitor. A series of 7-APPs was synthesized and evaluated for inhibitory activity against HCV in different cell culture systems. The synthesis and preliminary structure-activity relationship study of 7-APP are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2012.10.123