Research Topics
| Weiguo LiuSummaryAffiliation: Merck Research Laboratories Country: USA Publications
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Detail Information
Publications
Design, synthesis, and structure-activity relationship of podocarpic acid amides as liver X receptor agonists for potential treatment of atherosclerosisWeiguo 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...
Benzimidazolones: a new class of selective peroxisome proliferator-activated receptor γ (PPARγ) modulatorsWeiguo 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...
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemiaWeiguo 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...
Discovery and development of dimeric podocarpic acid leads as potent agonists of liver X receptor with HDL cholesterol raising activity in mice and hamstersSheo 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...
Highly functionalized 7-azaindoles as selective PPAR gamma modulatorsSheryl 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...
Structure-activity relationship of cytochrome bc1 reductase inhibitor broad spectrum antifungal ilicicolin HSheo 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...
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampinTawanda 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...
Isoniazid bactericidal activity and resistance emergence: integrating pharmacodynamics and pharmacogenomics to predict efficacy in different ethnic populationsTawanda 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....
Anidulafungin pharmacokinetics and microbial response in neutropenic mice with disseminated candidiasisTawanda 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...
Bacterial-population responses to drug-selective pressure: examination of garenoxacin's effect on Pseudomonas aeruginosaVincent H Tam
Emerging Infections and Host Defense Theme, Ordway Research Institute, Albany, NY 12208, USA
J Infect Dis 192:420-8. 2005....
Photodynamic therapy causes cross-linking of signal transducer and activator of transcription proteins and attenuation of interleukin-6 cytokine responsiveness in epithelial cellsWeiguo 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...
Intraocular concentration and pharmacokinetics of triamcinolone acetonide after a single intravitreal injectionPaul 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...
