Weiguo Liu

Summary

Affiliation: Merck Research Laboratories
Country: USA

Publications

  1. ncbi request reprint Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis
    Weiguo Liu
    Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:4574-8. 2005
  2. doi request reprint Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators
    Weiguo Liu
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, United States
    J Med Chem 54:8541-54. 2011
  3. doi request reprint Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia
    Weiguo Liu
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Med Chem 52:4443-53. 2009
  4. ncbi request reprint Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters
    Sheo B Singh
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:2824-8. 2005
  5. doi request reprint Highly functionalized 7-azaindoles as selective PPAR gamma modulators
    Sheryl D Debenham
    Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:4798-801. 2008
  6. doi request reprint Structure-activity relationship of cytochrome bc1 reductase inhibitor broad spectrum antifungal ilicicolin H
    Sheo B Singh
    Departments of Medicinal Chemistry and Infectious Disease, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA Electronic address
    Bioorg Med Chem Lett 23:3018-22. 2013
  7. pmc Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin
    Tawanda Gumbo
    Division of Infectious Diseases, University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 51:3781-8. 2007
  8. pmc Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populations
    Tawanda Gumbo
    Division of Infectious Diseases, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 51:2329-36. 2007
  9. pmc Anidulafungin pharmacokinetics and microbial response in neutropenic mice with disseminated candidiasis
    Tawanda Gumbo
    Division of Infectious Diseases, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 50:3695-700. 2006
  10. ncbi request reprint Bacterial-population responses to drug-selective pressure: examination of garenoxacin's effect on Pseudomonas aeruginosa
    Vincent H Tam
    Emerging Infections and Host Defense Theme, Ordway Research Institute, Albany, NY 12208, USA
    J Infect Dis 192:420-8. 2005

Collaborators

Detail Information

Publications12

  1. ncbi request reprint Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosis
    Weiguo Liu
    Merck Research Laboratories, P O Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:4574-8. 2005
    ..Compound 18 exhibited LXRalpha/beta 50/20 nM (binding affinity) and 33.7/35.3-fold receptor inductions. Synthesis, SAR, and biological activities of new podocarpate analogs are discussed...
  2. doi request reprint Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulators
    Weiguo Liu
    Merck Research Laboratories, P O Box 2000, Rahway, New Jersey 07065, United States
    J Med Chem 54:8541-54. 2011
    ..Side effects, such as fluid retention and heart weight gain associated with PPARγ full agonists, were diminished with 51 in comparison to rosiglitazone based on studies in two independent animal models...
  3. doi request reprint Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia
    Weiguo Liu
    Merck Research Laboratories, Rahway, New Jersey 07065, USA
    J Med Chem 52:4443-53. 2009
    ..The moderate PPARalpha activity of 12d not only contributed to the agent's ability to manage lipid profiles but also appears to have potentiated its PPARgamma efficacy in lowering glucose levels in preclinical diabetic animal models...
  4. ncbi request reprint Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamsters
    Sheo B Singh
    Merck Research Laboratories, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 15:2824-8. 2005
    ..An imide analog increased the level of HDL by 26%, decreased LDL by 10.6%, and increased triglyceride by 51% in hamsters. Discovery, synthesis, SAR and details of the activities of dimers have been described...
  5. doi request reprint Highly functionalized 7-azaindoles as selective PPAR gamma modulators
    Sheryl D Debenham
    Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA
    Bioorg Med Chem Lett 18:4798-801. 2008
    ..Addition of substituents at the 6-position of the 7-azaindoles improves in vitro potency and pharmacokinetics. 7-Azaindoles have significantly improved off-target profiles compared to the parent indole series...
  6. doi request reprint Structure-activity relationship of cytochrome bc1 reductase inhibitor broad spectrum antifungal ilicicolin H
    Sheo B Singh
    Departments of Medicinal Chemistry and Infectious Disease, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA Electronic address
    Bioorg Med Chem Lett 23:3018-22. 2013
    ..4',19-Diacetate and 19-cyclopropyl acetate retained antifungal and enzyme activity and selectivity with over 20-fold improvement of plasma protein binding...
  7. pmc Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin
    Tawanda Gumbo
    Division of Infectious Diseases, University of Texas Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 51:3781-8. 2007
    ..tuberculosis, (ii) the achievement of a free C(max)/MIC of >175 that can be tolerated by patients, and (iii) a long postantibiotic effect duration...
  8. pmc Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populations
    Tawanda Gumbo
    Division of Infectious Diseases, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 51:2329-36. 2007
    ....
  9. pmc Anidulafungin pharmacokinetics and microbial response in neutropenic mice with disseminated candidiasis
    Tawanda Gumbo
    Division of Infectious Diseases, UT Southwestern Medical Center, 5323 Harry Hines Blvd, Dallas, TX 75390 9113, USA
    Antimicrob Agents Chemother 50:3695-700. 2006
    ..This pharmacokinetic-pharmacodynamic picture of anidulafungin persistence in tissues and the resultant persistent fungal decline should be exploited to improve the efficacy of anidulafungin therapy for candidemia...
  10. ncbi request reprint Bacterial-population responses to drug-selective pressure: examination of garenoxacin's effect on Pseudomonas aeruginosa
    Vincent H Tam
    Emerging Infections and Host Defense Theme, Ordway Research Institute, Albany, NY 12208, USA
    J Infect Dis 192:420-8. 2005
    ....
  11. ncbi request reprint Photodynamic therapy causes cross-linking of signal transducer and activator of transcription proteins and attenuation of interleukin-6 cytokine responsiveness in epithelial cells
    Weiguo Liu
    Department of Molecular and Cellular Biology, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Cancer Res 64:6579-87. 2004
    ..It is suggested that the loss of responsiveness to these inflammatory cytokines in the PDT-treated field assists tumor cells in evading the growth-suppressive activity of these mediators expected to be present at tissue sites after PDT...
  12. ncbi request reprint Intraocular concentration and pharmacokinetics of triamcinolone acetonide after a single intravitreal injection
    Paul M Beer
    Department of Ophthalmology, Lions Eye Institute, Albany Medical College, Albany, New York, USA
    Ophthalmology 110:681-6. 2003
    ..To describe the pharmacokinetics occurring after the direct injection of triamcinolone acetonide into the vitreous humor of humans...