Gui Bai Liang

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. doi request reprint Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
    Gui Bai Liang
    Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:3706-10. 2008
  2. ncbi request reprint Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
    Tesfaye Biftu
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, P O Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 15:3296-301. 2005
  3. ncbi request reprint Synthesis and SAR studies of diarylpyrrole anticoccidial agents
    Xiaoxia Qian
    Merck Research Laboratories, Department of Medicinal Chemistry Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:2817-21. 2006
  4. ncbi request reprint (3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
    Tesfaye Biftu
    Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:49-52. 2007
  5. ncbi request reprint Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:1903-7. 2007
  6. ncbi request reprint Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry and Human and Animal Infectious Disease Research, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:4570-3. 2005
  7. doi request reprint N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:2019-22. 2008
  8. ncbi request reprint Synthesis and SAR studies of potent imidazopyridine anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:3558-61. 2007
  9. ncbi request reprint Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents
    Tesfaye Biftu
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:2479-83. 2006
  10. ncbi request reprint Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents
    Dennis Feng
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:5978-81. 2006

Detail Information

Publications11

  1. doi request reprint Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design
    Gui Bai Liang
    Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:3706-10. 2008
    ..These newly found binding elements were successfully incorporated into novel DPP-4 inhibitors...
  2. ncbi request reprint Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
    Tesfaye Biftu
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, P O Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 15:3296-301. 2005
    ..These compounds have a broad spectrum of activity. Based on the in vivo efficacy and cost of synthesis, the N-ethyl analog 23 was chosen as a novel anticoccidial agent for a field trial...
  3. ncbi request reprint Synthesis and SAR studies of diarylpyrrole anticoccidial agents
    Xiaoxia Qian
    Merck Research Laboratories, Department of Medicinal Chemistry Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:2817-21. 2006
    ..Further SAR studies on the side chain of the 2-pyrrolidine nitrogen did not enhance in vivo anticoccidial activity...
  4. ncbi request reprint (3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
    Tesfaye Biftu
    Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:49-52. 2007
    ..6nM), selective, and efficacious in an oral glucose tolerance test in mice. It was selected for extensive preclinical development as a potential back-up candidate to sitagliptin...
  5. ncbi request reprint Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:1903-7. 2007
    ..0 nM) and 3R,6R-dimethyl-1,4-diazepan-2-one derivative 14a (DPP-4 IC(50)=9.7 nM)...
  6. ncbi request reprint Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry and Human and Animal Infectious Disease Research, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:4570-3. 2005
    ..High potency in Et-PKG inhibition and broad-spectrum anticoccidial activities have been observed on compounds, such as 4b and 5h, which are fully efficacious in vivo at 50 ppm in feed...
  7. doi request reprint N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives with heterocyclic substitutions as potent and broad spectrum anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:2019-22. 2008
    ..Improvements in potency of Et-PKG inhibition, such as azetidine derivative 3a, and broad spectrum anticoccidial activities in feed, such as morpholine derivative 8c, have been achieved...
  8. ncbi request reprint Synthesis and SAR studies of potent imidazopyridine anticoccidial agents
    Gui Bai Liang
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 17:3558-61. 2007
    ..The most potent compounds are the 7-isopropylaminomethyl analog 6a and 2-isopropylamino analog 7i. These compounds are also fully active in in vivo assay as anticoccidial agents at 25 ppm in feed...
  9. ncbi request reprint Synthesis and SAR studies of very potent imidazopyridine antiprotozoal agents
    Tesfaye Biftu
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:2479-83. 2006
    ..However, both compounds are positive in the Ames microbial mutagenesis assay which precludes them from further development as antiprotozoal agents in the absence of negative lifetime rodent carcinogenicity studies...
  10. ncbi request reprint Synthesis and SAR of 2-(4-fluorophenyl)-3-pyrimidin-4-ylimidazo[1,2-a]pyridine derivatives as anticoccidial agents
    Dennis Feng
    Merck Research Laboratories, Department of Medicinal Chemistry, Merck and Co, Inc, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 16:5978-81. 2006
    ..Compounds 10a-10d and 10i are very potent inhibitors of Eimeria tenella cGMP-dependent protein kinase (0.081-0.32 nM) and are very efficacious antiparasitic agents in vivo when administered to chickens at 12.5-25 ppm levels in the feed...
  11. doi request reprint 3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists
    Shawn P Walsh
    Merck Research Laboratories, Merck and Co, Inc, 126 E Lincoln Ave, PO Box 2000, Rahway, NJ 07065 0900, USA
    Bioorg Med Chem Lett 21:3390-4. 2011
    ..Finally, further profiling of compound 7 is presented, including demonstration of enhanced glucose tolerance in an in vivo mouse model...