Charles Gluchowski

Publications (4)12.64 Total impact

• Article: ChemInform Abstract: 2Amino2-oxazolines as Subtype Selective α2 Adrenoceptor Agonists

  Wai C. Wong, Wanying Sun, Weili Cui, Yuewen Chen, Carlos Forray, Pierre J.-J. Vaysse, Theresa A. Branchek, Charles Gluchowski
  ChemInform 01/2010; 31(30).
• Article: Design and synthesis of an alpha1a-adrenergic receptor subtype-selective antagonist from BE2254.

  George Chiu, Charles Gluchowski, Carlos Forray
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  ABSTRACT: An alpha1a-adrenoceptor-selective antagonist has the potential to be a new benign prostatic hyperplasia drug with reduced side-effects. Modification of the non-selective antagonist BE2254 led to the development of a series of tetralin analogs. Evaluation of these compounds in cloned human alpha1-adrenoceptors resulted in the discovery of an analog that showed selectivity toward the human alpha1a-adrenergic receptor subtype. The compound also showed moderate potency to block human prostate muscle contraction.
  Chemical Biology &amp Drug Design 07/2006; 67(6):437-9. · 2.28 Impact Factor
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  Available from: tuwien.ac.at

  Article: Synthesis and structure-activity relationship of fluoro analogues of 8-{2-[4-(4-methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as selective alpha(1d)-adrenergic receptor antagonists.

  Michael J Konkel, John M Wetzel, Marie Cahir, Douglas A Craig, Stewart A Noble, Charles Gluchowski
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  ABSTRACT: We have discovered high-affinity antagonists (exemplified by 11 and 12) that are the most selective for alpha(1d)-adrenergic receptors (alpha(1d)-AR) reported to date. In cloned receptor assay systems, 12 displays at least 95-fold selectivity for the alpha(1d)-AR over all other G-protein-coupled receptors tested, and the subtype selectivity of 11 was confirmed in pharmacologically defined isolated tissue preparations.
  Journal of Medicinal Chemistry 05/2005; 48(8):3076-9. · 5.25 Impact Factor
• Article: High-throughput synthesis optimization of sulfonamide NPY Y5 antagonists.

  John Finn, David Pelham, Mary W Walker, Charles Gluchowski
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  ABSTRACT: A series of sulfonamide neuropeptide Y Y5 antagonists was optimized by preparation of sets of analogues using high-throughput synthesis and purification techniques. Testing of these compounds for their ability to bind to the human NPY Y5 receptor revealed separate SAR trends for sulfonamide amides versus sulfonamide ureas versus sulfonamide amines. By understanding these SAR trends, potent compounds were identified in all three series.
  Bioorganic & Medicinal Chemistry Letters 08/2002; 12(13):1771-4. · 2.55 Impact Factor
• Article: Discovery of potent and selective small molecule NPY Y5 receptor antagonists.

  Imadul Islam, Dale Dhanoa, John Finn, Ping Du, Mary W Walker, John A Salon, Jack Zhang, Charles Gluchowski
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  ABSTRACT: The discovery of a new class of sulfonamide NPY Y5 receptor antagonists is described. Optimization of this series led to the identification of compounds with high affinity for the hY5 subtype and excellent selectivity over the other NPY receptor subtypes. The SAR for this series was examined and a model for understanding the ligand-receptor interactions was developed.
  Bioorganic & Medicinal Chemistry Letters 08/2002; 12(13):1767-9. · 2.55 Impact Factor
• Article: 2Amino2-oxazolines as Subtype Selective α 2 Adrenoceptor Agonists

  Wai C. Wong, Wanying Sun, Weili Cui, Yuewen Chen, Carlos Forray, Pierre J.-J. Vaysse, Theresa A. Branchek, Charles Gluchowski
  Journal of Medicinal Chemistry - J MED CHEM. 01/2000; 43(9):1699-1704.