Hratch Zokian

Publications (4)10.6 Total impact

• Article: Substituted phenyl triazoles as selective inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1.

  Wanying Sun, Milana Maletic, Steven S Mundt, Kashmira Shah, Hratch Zokian, Kathy Lyons, Sherman T Waddell, James Balkovec
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  ABSTRACT: 3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (HSD1). They were shown to be active in the mouse in vivo pharmacodynamic model (PD) for HSD1 but exhibited a potent off-target activation of the Pregnane X Receptor (PXR). SAR studies and synthesis of analogs that led to the discovery of a selective HSD1 inhibitor are described in detail.
  Bioorganic & medicinal chemistry letters 02/2011; 21(7):2141-5. · 2.65 Impact Factor
• Article: 4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

  Yuping Zhu, Steven H Olson, Anne Hermanowski-Vosatka, Steven Mundt, Kashmira Shah, Marty Springer, Rolf Thieringer, Samuel Wright, Jianying Xiao, Hratch Zokian, James M Balkovec
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  ABSTRACT: 4-Methyl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They were active in vitro and in an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.
  Bioorganic & medicinal chemistry letters 07/2008; 18(11):3405-11. · 2.65 Impact Factor
• Article: Phenylcyclobutyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.

  Yuping Zhu, Steven H Olson, Donald Graham, Gool Patel, Anne Hermanowski-Vosatka, Steven Mundt, Kashmira Shah, Marty Springer, Rolf Thieringer, Samuel Wright, Jianying Xiao, Hratch Zokian, Jasminka Dragovic, James M Balkovec
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  ABSTRACT: 3-(Phenylcyclobutyl)-1,2,4-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). These were active both in vitro and in an in vivo mouse pharmacodynamic (PD) model. Fluorine substitution of the cyclobutane ring improved the pharmacokinetic profile significantly. The synthesis and structure-activity relationships are presented.
  Bioorganic & medicinal chemistry letters 07/2008; 18(11):3412-6. · 2.65 Impact Factor
• Article: Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.

  Susan D Aster, Donald W Graham, Divya Kharbanda, Gool Patel, Mitree Ponpipom, Gina M Santorelli, Michael J Szymonifka, Steven S Mundt, Kashmira Shah, Marty S Springer, Rolf Thieringer, Anne Hermanowski-Vosatka, Samuel D Wright, Jianying Xiao, Hratch Zokian, James M Balkovec
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  ABSTRACT: 3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.
  Bioorganic & medicinal chemistry letters 06/2008; 18(9):2799-804. · 2.65 Impact Factor