Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: Identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole

Ishida, Tomio; Suzuki, Takayoshi; Hirashima, Shin‐ichi; Mizutani, Kenji; Yoshida, Akinori; Ando, Izuru; Ikeda, Satoru; Adachi, Tsutomu; Hashimoto, Harukichi

doi:10.1016/j.bmcl.2006.01.032

Cited by 123 publications

(59 citation statements)

References 17 publications

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“…Nonnucleoside polymerase inhibitors (NNIs) interact with four distinct allosteric sites on HCV polymerase (4). We previously reported the discovery of several HCV polymerase inhibitors with a benzimidazole and indole core based on highthroughput screening and structure-based drug design (14,15,18,19).…”

Section: H Epatitis C Virus (Hcv) Is the Major Cause Of Posttransfusimentioning

confidence: 99%

Preclinical Characterization of JTK-853, a Novel Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

Ando

Adachi

Ogura

et al. 2012

Antimicrob Agents Chemother

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Section: H Epatitis C Virus (Hcv) Is the Major Cause Of Posttransfusimentioning

confidence: 99%

Preclinical Characterization of JTK-853, a Novel Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

Ando

Adachi

Ogura

et al. 2012

Antimicrob Agents Chemother

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“…Binding of inhibitors to NNI-1 is purported to displace the flexible 1 loop from its thumb domain binding site, perturbing the interaction between the NS5B polymerase finger and thumb domains and thereby locking the enzyme in an open inactive conformation. Small molecules with benzimidazole (4,16,41) and indole chemical scaffolds (15) were identified as NNI-1-directed NS5B inhibitors.…”

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confidence: 99%

TMC647055, a Potent Nonnucleoside Hepatitis C Virus NS5B Polymerase Inhibitor with Cross-Genotypic Coverage

Devogelaere

Berke

Vijgen

et al. 2012

Antimicrob Agents Chemother

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ABSTRACTHepatitis C virus (HCV) infection is a major global health burden and is associated with an increased risk of liver cirrhosis and hepatocellular carcinoma. There remains an unmet medical need for efficacious and safe direct antivirals with complementary modes of action for combination in treatment regimens to deliver a high cure rate with a short duration of treatment for HCV patients. Here we report thein vitroinhibitory activity, mode of action, binding kinetics, and resistance profile of TMC647055, a novel and potent nonnucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase.In vitrocombination studies with an HCV NS3/4A protease inhibitor demonstrated potent suppression of HCV RNA replication, confirming the potential for combination of these two classes in the treatment of chronic HCV infection. TMC647055 is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication with a promisingin vitrobiochemical, kinetic, and virological profile that is currently undergoing clinical evaluation.

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“…In terms of this trend, the literature survey showed that indole derivatives possess anticancer [16,17], antioxidant [18], antibacterial [19], antifungal [20,21], antiviral [22,23], and antihypertensive activities [24]. Indole-3-carbon atom in the form of spiro carbon atom exhibits enhanced biological activities [25,26].…”

Section: Introductionmentioning

confidence: 99%

Environ-Economic Synthesis and Characterization of Some New 1,2,4-Triazole Derivatives as Organic Fluorescent Materials and Potent Fungicidal Agents

Sachdeva

Saroj

Khaturia

et al. 2013

Organic Chemistry International

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A multicomponent one-pot clean cyclocondensation reaction of 4-chloro-2-nitro aniline/amino acids and aromatic aldehydes/ indole-2,3-diones with thiosemicarbazide in water yielding triazole/spiro indole-triazole derivatives in high yields and shorter reaction time and displaying excellent florescent property is reported. The developed MCR may provide a valuable practical tool for the synthesis of new drugs containing the title core fragment. All the newly synthesized compounds have been characterized by IR, 1 HNMR, 13 CNMR, and fluorescence study and also been screened for antimicrobial activity.

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Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: Identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole

Cited by 123 publications

References 17 publications

Preclinical Characterization of JTK-853, a Novel Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

Preclinical Characterization of JTK-853, a Novel Nonnucleoside Inhibitor of the Hepatitis C Virus RNA-Dependent RNA Polymerase

TMC647055, a Potent Nonnucleoside Hepatitis C Virus NS5B Polymerase Inhibitor with Cross-Genotypic Coverage

Environ-Economic Synthesis and Characterization of Some New 1,2,4-Triazole Derivatives as Organic Fluorescent Materials and Potent Fungicidal Agents

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