Hua Wang

Publications (4)10.41 Total impact

• Article: Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.

  Joseph Pontillo, Dongpei Wu, Brett Ching, Sarah Hudson, Marc J Genicot, Yinghong Gao, Todd Ewing, Beth A Fleck, Kathleen Gogas, Anna Aparicio, Hua Wang, Jenny Wen, Warren S Wade
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  ABSTRACT: The design synthesis and SAR of a series of chiral ring-constrained norepinephrine reuptake inhibitors with improved physicochemical properties is described. Typical compounds are potent (IC(50)s<10 nM), selective against the other monoamine transporters, weak CYP2D6 inhibitors (IC(50)s>1 microM) and stable to oxidation by human liver microsomes. In addition, the compounds exhibit a favorable polarity profile.
  Bioorganic & medicinal chemistry letters 12/2008; 18(23):6151-5. · 2.65 Impact Factor
• Article: Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.

  Sarah Hudson, Mehrak Kiankarimi, Wendy Eccles, Wesley Dwight, Yalda S Mostofi, Marc J Genicot, Beth A Fleck, Kathleen Gogas, Anna Aparicio, Hua Wang, Jenny Wen, Warren S Wade
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  ABSTRACT: The synthesis and SAR of a series of chiral heterocyclic ring-constrained norepinephrine reuptake inhibitors are described. The best compounds compare favorably with atomoxetine in potency (IC(50)s<10 nM), selectivity against the other monoamine transporters, and inhibition of CYP2D6 (IC(50)s>1 microM). In addition, the compounds are generally more stable than atomoxetine to oxidative metabolism and thus are likely to have lower clearance in humans.
  Bioorganic & medicinal chemistry letters 08/2008; 18(16):4491-4. · 2.65 Impact Factor
• Article: Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).

  Martin W Rowbottom, Troy D Vickers, Junko Tamiya, Mingzhu Zhang, Brian Dyck, Jonathan Grey, David Schwarz, Christopher E Heise, Michael Hedrick, Jenny Wen, Hui Tang, Hua Wang, Andrew Fisher, Anna Aparicio, John Saunders, Val S Goodfellow
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  ABSTRACT: The design, synthesis, and SAR of a series of substituted spirohydantoins are described. Optimization of an in-house screening hit gave compounds that exhibited potent binding affinity and functional activity at MCH-R1.
  Bioorganic & Medicinal Chemistry Letters 05/2007; 17(8):2171-8. · 2.55 Impact Factor
• Article: Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.

  Sarah Hudson, Mehrak Kiankarimi, Martin W Rowbottom, Troy D Vickers, Dongpei Wu, Joseph Pontillo, Brett Ching, Wesley Dwight, Val S Goodfellow, David Schwarz, Christopher E Heise, Ajay Madan, Jenny Wen, William Ban, Hua Wang, Warren S Wade
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  ABSTRACT: The design, synthesis, and SAR of a series of retro bis-aminopyrrolidine ureas are described. Compounds from this series exhibited considerable binding affinity (Ki = 1 nM) and functional activity at MCH-R1, acceptable CYP2D6 inhibition, and good rat brain exposure.
  Bioorganic & Medicinal Chemistry Letters 10/2006; 16(18):4922-30. · 2.55 Impact Factor