Literature DB >> 19819138

Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase.

Janeta Popovici-Muller1, Gerald W Shipps, Kristin E Rosner, Yongqi Deng, Tong Wang, Patrick J Curran, Meredith A Brown, M Arshad Siddiqui, Alan B Cooper, José Duca, Michael Cable, Viyyoor Girijavallabhan.   

Abstract

The present paper describes a novel series of HCV RNA polymerase inhibitors based on a pyrazolo[1,5-a]pyrimidine scaffold bearing hydrophobic groups and an acidic functionality. Several compounds were optimized to low nanomolar potencies in a biochemical RdRp assay. SAR trends clearly reveal a stringent preference for a cyclohexyl group as one of the hydrophobes, and improved activities for carboxylic acid derivatives.

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Year:  2009        PMID: 19819138     DOI: 10.1016/j.bmcl.2009.09.087

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

1.  Synthesis, Structural Elucidation, and In Vitro Antitumor Activities of Some Pyrazolopyrimidines and Schiff Bases Derived from 5-Amino-3-(arylamino)-1H-pyrazole-4-carboxamides.

Authors:  Taghrid S Hafez; Souad A Osman; Hisham Abdallah A Yosef; Amira S Abd El-All; Ashraf S Hassan; Abdallah A El-Sawy; Mohamed M Abdallah; Mahmoud Youns
Journal:  Sci Pharm       Date:  2013-01-03

Review 2.  DNMT3A and IDH mutations in acute myeloid leukemia and other myeloid malignancies: associations with prognosis and potential treatment strategies.

Authors:  A P Im; A R Sehgal; M P Carroll; B D Smith; A Tefferi; D E Johnson; M Boyiadzis
Journal:  Leukemia       Date:  2014-04-04       Impact factor: 12.883

3.  Anti-inflammatory and antimicrobial activities of novel pyrazole analogues.

Authors:  R Surendra Kumar; Ibrahim A Arif; Anis Ahamed; Akbar Idhayadhulla
Journal:  Saudi J Biol Sci       Date:  2015-07-29       Impact factor: 4.219

4.  Synthesis and characterization of celecoxib derivatives as possible anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV agents.

Authors:  Ş Güniz Küçükgüzel; İnci Coşkun; Sevil Aydın; Göknur Aktay; Şule Gürsoy; Özge Çevik; Özlem Bingöl Özakpınar; Derya Özsavcı; Azize Şener; Neerja Kaushik-Basu; Amartya Basu; Tanaji T Talele
Journal:  Molecules       Date:  2013-03-21       Impact factor: 4.411

  4 in total

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