Literature DB >> 15993055

Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.

Helmut Haning1, Ulrich Niewöhner, Thomas Schenke, Thomas Lampe, Alexander Hillisch, Erwin Bischoff.   

Abstract

Several different heterocyclic systems were compared as PDE5 inhibitor scaffolds. In addition to the known 3H-imidazo[5,1-f][1,2,4]triazin-4-ones and pyrazolopyrimidinones, isomeric imidazo[1,5-a][1,3,5]triazin-4(3H)-ones were also shown to be potent and selective PDE inhibitor scaffolds with in vivo activity. SAR trends were elucidated for sulfonamide derivatives with generality across different scaffolds.

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Year:  2005        PMID: 15993055     DOI: 10.1016/j.bmcl.2005.05.090

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


  3 in total

1.  Novel Pieces for the Emerging Picture of Sulfoximines in Drug Discovery: Synthesis and Evaluation of Sulfoximine Analogues of Marketed Drugs and Advanced Clinical Candidates.

Authors:  Juan Alberto Sirvent; Ulrich Lücking
Journal:  ChemMedChem       Date:  2017-03-22       Impact factor: 3.466

2.  A one-pot, multicomponent reaction for the synthesis of novel 2-alkyl substituted 4-aminoimidazo[1,2-a][1,3,5]triazines.

Authors:  Felicia Phei Lin Lim; Lin Yuing Tan; Edward R T Tiekink; Anton V Dolzhenko
Journal:  RSC Adv       Date:  2018-06-12       Impact factor: 3.361

3.  An easy synthesis of 5-functionally substituted ethyl 4-amino-1-aryl- pyrazolo-3-carboxylates: interesting precursors to sildenafil analogues.

Authors:  Said A S Ghozlan; Khadija O Badahdah; Ismail A Abdelhamid
Journal:  Beilstein J Org Chem       Date:  2007-05-01       Impact factor: 2.883

  3 in total

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