Xiaobing Li

Publications (7)19.77 Total impact

• Article: Efficient conversion of Biginelli 3,4-dihydropyrimidin-2(1H)-one to pyrimidines via PyBroP-mediated coupling.

  Fu-An Kang, Jason Kodah, Qunying Guan, Xiaobing Li, William V Murray
  [show abstract] [hide abstract]
  ABSTRACT: An efficient two-step procedure is described to convert the Biginelli 3,4-dihydropyrimidin-2(1H)-one to various multifunctionalized pyrimidines via the Kappe dehydrogenation and a new mild PyBroP-mediated coupling with C, N, O, and S nucleophiles, which provides a readily accessible multifunctionalized pyrimidine template for diversity-oriented synthesis.
  The Journal of Organic Chemistry 04/2005; 70(5):1957-60. · 4.45 Impact Factor
• Article: Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.

  Laura C McAtee, Steven W Sutton, Dale A Rudolph, Xiaobing Li, Leah E Aluisio, Victor K Phuong, Curt A Dvorak, Timothy W Lovenberg, Nicholas I Carruthers, Todd K Jones
  [show abstract] [hide abstract]
  ABSTRACT: Orexins, also termed hypocretins, consist of two neuropeptide agonists (orexin A and B) interacting with two known G-protein coupled receptors (OX(1)R and OX(2)R). In addition to other biological functions, the orexin-2 receptor is thought to be an important modulator of sleep and wakefulness. Herein we describe a series of novel, selective OX(2)R antagonists consisting of substituted 4-phenyl-[1,3]dioxanes. One such antagonist is compound 9, 1-(2,4-dibromo-phenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)-urea, which is bound by the OX(2)R with a pK(i) of 8.3, has a pK(b) of 7.9, and is 600-fold selective for the OX(2)R over the OX(1)R.
  Bioorganic & Medicinal Chemistry Letters 09/2004; 14(16):4225-9. · 2.55 Impact Factor
• Article: Novel non-peptidic neuropeptide Y Y2 receptor antagonists.

  Jill A Jablonowski, Wenying Chai, Xiaobing Li, Dale A Rudolph, William V Murray, Mark A Youngman, Scott L Dax, Diane Nepomuceno, Pascal Bonaventure, Timothy W Lovenberg, Nicholas I Carruthers
  [show abstract] [hide abstract]
  ABSTRACT: Through SAR studies of a piperidinylindoline cinnamide HTS lead, the first potent, non-peptide, low molecular weight selective Neuropeptide Y Y2 (NPY Y2) antagonists have been synthesized. The SAR studies around the piperidinyl, the indolinyl, and the cinnamyl moieties are discussed.
  Bioorganic & Medicinal Chemistry Letters 04/2004; 14(5):1239-42. · 2.55 Impact Factor
• Article: Non-imidazole heterocyclic histamine H3 receptor antagonists.

  Wenying Chai, J Guy Breitenbucher, Annette Kwok, Xiaobing Li, Victoria Wong, Nicholas I Carruthers, Timothy W Lovenberg, Curt Mazur, Sandy J Wilson, Frank U Axe, Todd K Jones
  [show abstract] [hide abstract]
  ABSTRACT: Continued exploration of the SAR around the lead imidazopyridine histamine H(3) antagonist 1 has led to the discovery of several related series of heterocyclic histamine H(3) antagonists. The synthesis and SAR of indolizine, indole and pyrazolopyridine based compounds are now described.
  Bioorganic & Medicinal Chemistry Letters 06/2003; 13(10):1767-70. · 2.55 Impact Factor
• Article: Novel human histamine H(3) receptor antagonists.

  Chandra Shah, Laura McAtee, J Guy Breitenbucher, Dale Rudolph, Xiaobing Li, Timothy W Lovenberg, Curt Mazur, Sandy J Wilson, Nicholas I Carruthers
  [show abstract] [hide abstract]
  ABSTRACT: High throughput screening, using the recombinant human H(3) receptor, was used to identify novel histamine H(3) receptor antagonists. Evaluation of the lead compounds ultimately afforded potent, selective, orally bioavailable compounds (e.g., 38) with favorable blood-brain barrier penetration.
  Bioorganic & Medicinal Chemistry Letters 12/2002; 12(22):3309-12. · 2.55 Impact Factor
• Article: Arylpiperazine substituted heterocycles as selective alpha(1a) adrenergic antagonists.

  Haripada Khatuya, Richard H Hutchings, Gee-Hong Kuo, Virginia L Pulito, Linda K Jolliffe, Xiaobing Li, William V Murray
  [show abstract] [hide abstract]
  ABSTRACT: Antagonists of the alpha(1)-adrenergic receptors (alpha(1)-ARs) are useful for the treatment of benign prostatic hyperplasia. A series of potent and subtype-selective alpha(1a)-AR antagonists has been synthesized, displaying in vitro binding affinity in the low the nanomolar range.
  Bioorganic & Medicinal Chemistry Letters 10/2002; 12(17):2443-6. · 2.55 Impact Factor
• Article: Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.

  Haripada Khatuya, Virginia L Pulito, Linda K Jolliffe, Xiaobing Li, William V Murray
  [show abstract] [hide abstract]
  ABSTRACT: The syntheses and biological activities of a novel series of 2,4- and 2,5-disubstituted thiophenes are reported. These analogues have shown excellent affinity and selectivity against alpha(1)-adrenoreceptor subtypes.
  Bioorganic & Medicinal Chemistry Letters 09/2002; 12(16):2145-8. · 2.55 Impact Factor