Author: Song, Zhiguo Jake ; Alam, Mahbub ; Li, Hongming ; Morris, William J. ; Limanto, John ; Yasuda, Nobuyoshi ; Thaisrivongs, David A. ; Cohen, Ryan D. ; Cleator, Ed ; Tan, Lushi ; Liu, Zhijian ; Yin, Jingjun ; Zhong, Yong-Li ; Bishop, Brian ; Mullens, Peter ; Shevlin, Michael ; Yin, Jianguo ; Campos, Kevin R. ; Goodyear, Adrian ; Dumas, Aaron M. ; Davies, Antony ; Sherer, Edward C. ; Edwards, John

An asymmetric synthesis of HCV NS5B nucleoside polymerase inhibitor (1) is described. This novel route features several remarkably diastereoselective and high-yielding transformations, including construction of the all-carbon quaternary stereogenic center at C-2 via a thermodynamic aldol reaction. A subsequent glycosylation reaction with activated uracil via C-1 phosphate and installation of the cyclic phosphate group using an achiral phosphorus(III) reagent followed by oxidation provides 1.

01 Nov 2010·Current Medicinal ChemistryQ2 · MEDICINE

NS5B RNA Dependent RNA Polymerase Inhibitors: The Promising Approach to Treat Hepatitis C Virus Infections

Q2 · MEDICINE

Review

Author: Deore, R. R. ; Chern, J.-W.

Hepatitis C virus (HCV), a causative agent for non-A and non-B hepatitis, has infected approximately 3% of world's population. The current treatment option of ribavirin in combination with pegylated interferon possesses lower sustained virological response rates, and has serious disadvantages. Unfortunately, no prophylactic vaccine has been approved yet. Therefore, there is an unmet clinical need for more effective and safe anti-HCV drugs. HCV NS5B RNA dependent RNA polymerase is currently pursued as the most popular target to develop safe anti-HCV agents, as it is not expressed in uninfected cells. More than 25 pharmaceutical companies and some research groups have developed ≈50 structurally diverse scaffolds to inhibit NS5B. Here we provide comprehensive account of the drug development process of these scaffolds. NS5B polymerase inhibitors have been broadly classified in nucleoside and non nucleoside inhibitors and are sub classified according to their mechanism of action and structural diversities. With some additional considerations about the inhibitor bound NS5B enzyme X-ray crystal structure information and pharmacological aspects of the inhibitors, this review summarizes the lead identification, structure activity relationship (SAR) studies leading to the most potent NS5B inhibitors with subgenomic replicon activity.

100 Deals associated with NS5B HCV RNA polymerase nucleoside inhibitors(Aviragen Therapeutics)

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis C	Discovery	Germany	Boehringer Ingelheim International GmbH	-
Hepatitis C	Discovery	Germany	Boehringer Ingelheim International GmbH	-
Hepatitis C	Discovery	United Kingdom	GSK Plc	-
Hepatitis C	Discovery	Australia	Aviragen Therapeutics, Inc.	-
Hepatitis C	Discovery	United Kingdom	GSK Plc	-
Hepatitis C	Discovery	Australia	Aviragen Therapeutics, Inc.	-

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NS5B HCV RNA polymerase nucleoside inhibitors(Aviragen Therapeutics)

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