Elfatih Elzein

Summary

Affiliation: CV Therapeutics
Country: USA

Publications

  1. ncbi Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 16:302-6. 2006
  2. ncbi Novel inhibitors of fatty acid oxidation as potential metabolic modulators
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:973-7. 2004
  3. ncbi 2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, California 94304, USA
    J Med Chem 47:4766-73. 2004
  4. ncbi Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    J Med Chem 51:2267-78. 2008
  5. ncbi N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 17:161-6. 2007
  6. ncbi CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics, Inc, 3172 Porter Dr, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:6017-21. 2004
  7. ncbi Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists
    Rao V Kalla
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, California 94304, USA
    J Med Chem 49:3682-92. 2006
  8. ncbi Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines
    Rao V Kalla
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 18:1397-401. 2008
  9. ncbi Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents
    Christopher F Morrison
    Department of Bioorganic Chemistry, CV Therapeutics, Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:3793-7. 2004
  10. ncbi New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties
    Dmitry O Koltun
    Department of Bioorganic Chemistry, 3172 Porter Dr, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:549-52. 2004

Detail Information

Publications11

  1. ncbi Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 16:302-6. 2006
    ..The synthesis and SAR of this novel class of compounds are presented herein...
  2. ncbi Novel inhibitors of fatty acid oxidation as potential metabolic modulators
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:973-7. 2004
    ....
  3. ncbi 2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, California 94304, USA
    J Med Chem 47:4766-73. 2004
    ....
  4. ncbi Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    J Med Chem 51:2267-78. 2008
    ..In a single ascending-dose phase I clinical study, compound 62 had no serious adverse events and was well tolerated...
  5. ncbi N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 17:161-6. 2007
    ..In addition, compound 19 that incorporated a carboxamide functionality in the 4-position of the pyrazole ring displayed subnanomolar affinity for the A(1)-AdoR (K(iL)=0.6 nM) and >600-fold selectivity over the A(3) and A(2A)-AdoRs...
  6. ncbi CVT-4325: a potent fatty acid oxidation inhibitor with favorable oral bioavailability
    Elfatih Elzein
    Department of Bioorganic Chemistry, CV Therapeutics, Inc, 3172 Porter Dr, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:6017-21. 2004
    ..SAR studies led to the discovery of CVT-4325 (shown), a potent FOXi (IC50=380 nM rat mitochondria) with favorable PK properties (F=93%, t(1/2)=13.6h, dog)...
  7. ncbi Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists
    Rao V Kalla
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, California 94304, USA
    J Med Chem 49:3682-92. 2006
    ....
  8. ncbi Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines
    Rao V Kalla
    Department of Bioorganic Chemistry, CV Therapeutics Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 18:1397-401. 2008
    ..CVT-6694 has been shown to block the release of interleukin-6 and monocyte chemotactic protein-1 from bronchial smooth muscle cells (BSMC), a process believed to be promoted by activation of A(2B) AdoR...
  9. ncbi Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents
    Christopher F Morrison
    Department of Bioorganic Chemistry, CV Therapeutics, Inc, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:3793-7. 2004
    ..Additional affinity, GTPgammaS binding data suggesting partial activity of the A(1) adenosine receptor, and PK results for 5(') modified adenosine derivatives are shown...
  10. ncbi New fatty acid oxidation inhibitors with increased potency lacking adverse metabolic and electrophysiological properties
    Dmitry O Koltun
    Department of Bioorganic Chemistry, 3172 Porter Dr, Palo Alto, CA 94304, USA
    Bioorg Med Chem Lett 14:549-52. 2004
    ..Compound 33 was also found to have favorable pharmacokinetic properties in rat...
  11. ncbi A1 adenosine receptor agonists and their potential therapeutic applications
    Elfatih Elzein
    CV Therapeutics, Inc, Department of Bioorganic Chemistry, 3172 Porter Drive, Palo Alto, CA 94304, USA
    Expert Opin Investig Drugs 17:1901-10. 2008
    ..A(1)-AdoR de-sensitization leading to tachyphylaxis is also another challenge...