Search: onr:"swepub:oai:DiVA.org:uu-199464" >
Structure-Based Dis...
Structure-Based Discovery of Pyrazolobenzothiazine Derivatives As Inhibitors of Hepatitis C Virus Replication
-
Barreca, Maria Letizia (author)
-
Manfroni, Giuseppe (author)
-
Leyssen, Pieter (author)
-
show more...
-
- Winquist, Johan (author)
- Uppsala universitet,Institutionen för kemi - BMC
-
Kaushik-Basu, Neerja (author)
-
Paeshuyse, Jan (author)
-
Krishnan, Ramalingam (author)
-
Iraci, Nunzio (author)
-
Sabatini, Stefano (author)
-
Tabarrini, Oriana (author)
-
Basu, Amartya (author)
-
- Danielson, U. Helena (author)
- Uppsala universitet,Biokemi
-
Neyts, Johan (author)
-
Cecchetti, Violetta (author)
-
show less...
-
(creator_code:org_t)
- 2013-03-07
- 2013
- English.
-
In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 56:6, s. 2270-2282
- Related links:
-
https://europepmc.or...
-
show more...
-
https://urn.kb.se/re...
-
https://doi.org/10.1...
-
show less...
Abstract
Subject headings
Close
- The NS5B RNA-dependent RNA polymerase is an attractive target for the development of novel and selective inhibitors of hepatitis C virus replication. To identify novel structural hits as anti-HCV agents, we performed structure based virtual screening of our in-house library followed by rational drug design, organic synthesis, and biological testing. These studies led to the identification of pyrazolobenzothiazine scaffold as a suitable template for obtaining novel anti-HCV agents targeting the NS5B polymerase. The best compound of this series was the meta-fluoro-N-1-phenyl pyrazolobenzothiazine derivative 4a, which exhibited an EC50 = 3.6 mu M, EC90 = 25.6 mu M, and CC50 > 180 mu M in the Huh 9-13 replicon system, thus providing a good starting point for further hit evolution.
Publication and Content Type
- ref (subject category)
- art (subject category)
Find in a library
To the university's database
- By the author/editor
-
Barreca, Maria L ...
-
Manfroni, Giusep ...
-
Leyssen, Pieter
-
Winquist, Johan
-
Kaushik-Basu, Ne ...
-
Paeshuyse, Jan
-
show more...
-
Krishnan, Ramali ...
-
Iraci, Nunzio
-
Sabatini, Stefan ...
-
Tabarrini, Orian ...
-
Basu, Amartya
-
Danielson, U. He ...
-
Neyts, Johan
-
Cecchetti, Viole ...
-
show less...
- Articles in the publication
-
Journal of Medic ...
- By the university
-
Uppsala University