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N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide

Names

[ CAS No. ]:
351438-49-8

[ Name ]:
N-(4-cyanophenyl)-5-(thiophen-2-yl)-7-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-2-carboxamide

[Synonym ]:
2-[(5-Methyl-5H-[1,2,4]triazino[5,6-b]indol-3-yl)sulfanyl]-N-[3-(trifluoromethyl)phenyl]acetamide
Acetamide, 2-[(5-methyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-[3-(trifluoromethyl)phenyl]-

Biological Activity

[Description]:

H1PVAT is a potent and selective inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), and inhibits early stage of the replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation[1][2].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Others >> Others

[Target]

EC50: 10 nM (PV-1), 26 nM (PV-2), 218 nM (PV-3)[1]


[In Vitro]

H1PVAT (10-218 nM; 24-48 h) inhibits poliovirus strain Sabin replication in a dose-dependent manner, with EC50s of 10 nM (PV-1), 26 nM (PV-2) and 218 nM (PV-3), respectively[1]. H1PVAT (30 min prior to or 1 h after PV-1 infection; 7 h) inhibits an early stage of viral replication , and only H1PVAT is administered prior to infection results reduction (>99.9%) in intracellular viral RNA levels[1]. H1PVAT (50 μM; 2 min) protects PV against heat inactivation with the 50% thermal inactivation temperature increased to 52.6 ℃ and 50.8 ℃, which suggests a direct interaction between the viral capsid and H1PVAT[1].

[References]

[1]. Tijsma A, et al. H1PVAT is a novel and potent early-stage inhibitor of poliovirus replication that targets VP1. Antiviral Res. 2014 Oct;110:1-9.

[2]. Tijsma A. Antiviral strategies against polio and other enteroviruses. 2018.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C19H14F3N5OS

[ Molecular Weight ]:
417.408

[ Exact Mass ]:
417.087128

[ LogP ]:
4.29

[ Index of Refraction ]:
1.674


Related Compounds