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Träfflista för sökning "WFRF:(Agback Tatiana) srt2:(2010-2014)"

Sökning: WFRF:(Agback Tatiana) > (2010-2014)

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1.
  • Nilsson, Magnus, et al. (författare)
  • Discovery of 4 '-azido-2 '-deoxy-2 '-C-methyl cytidine and prodrugs thereof : A potent inhibitor of Hepatitis C virus replication
  • 2012
  • Ingår i: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 22:9, s. 3265-3268
  • Tidskriftsartikel (refereegranskat)abstract
    • 4'-Azido-2'-deoxy-2'-methylcytidine (14) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC50 value of 1.2 mu M and showing moderate in vivo bioavailability in rat (F = 14%). Here we describe the synthesis and biological evaluation of 4'-azido-2'-deoxy-2'-methylcytidine and prodrug derivatives thereof. (C) 2012 Elsevier Ltd. All rights reserved.
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2.
  • Nilsson, Magnus, et al. (författare)
  • Synthesis and SAR of potent inhibitors of the Hepatitis C virus NS3/4A protease : Exploration of P2 quinazoline substituents
  • 2010
  • Ingår i: Bioorganic & Medicinal Chemistry Letters. - : Elsevier BV. - 0960-894X .- 1464-3405. ; 20:14, s. 4004-4011
  • Tidskriftsartikel (refereegranskat)abstract
    • Novel NS3/4A protease inhibitors comprising quinazoline derivatives as P2 substituent were synthesized. High potency inhibitors displaying advantageous PK properties have been obtained through the optimization of quinazoline P2 substituents in three series exhibiting macrocyclic P2 cyclopentane dicarboxylic acid and P2 proline urea motifs. For the quinazoline moiety it was found that 8-methyl substitution in the P2 cyclopentane dicarboxylic acid series improved on the metabolic stability in human liver microsomes. By comparison, the proline urea series displayed advantageous Caco-2 permeability over the cyclopentane series. Pharmacokinetic properties in vivo were assessed in rat on selected compounds, where excellent exposure and liver-to-plasma ratios were demonstrated for a member of the 14-membered quinazoline substituted P2 proline urea series. (C) 2010 Elsevier Ltd. All rights reserved.
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3.
  • Sandgren, Veronica, et al. (författare)
  • Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core : Design, synthesis and X-ray crystal structures of enzyme inhibitor complexes
  • 2012
  • Ingår i: Bioorganic & Medicinal Chemistry. - : Elsevier. - 0968-0896 .- 1464-3391. ; 29:14, s. 4377-4389
  • Tidskriftsartikel (refereegranskat)abstract
    • A series of P1-P3 linked macrocyclic BACE-1 inhibitors containing a hydroxyethylamine (HEA) isostere scaffold has been synthesized. All inhibitors comprise a toluene or N-phenylmethanesulfonamide P2 moiety. Excellent BACE-1 potencies, both in enzymatic and cell-based assays, were observed in this series of target compounds, with the best candidates displaying cell-based IC50 values in the low nanomolar range. As an attempt to improve potency, a phenyl substituent aiming at the S3 subpocket was introduced in the macrocyclic ring. X-ray analyses were performed on selected compounds, and enzyme-inhibitor interactions are discussed.
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  • Resultat 1-3 av 3

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