Search Results - "HUEBERT, Norman"

Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists by Song, Fengbin, Xu, Guozhang, Gaul, Michael D., Zhao, Baoping, Lu, Tianbao, Zhang, Rui, DesJarlais, Renee L., DiLoreto, Karen, Huebert, Norman, Shook, Brian, Rentzeperis, Dennis, Santulli, Rosie, Eckardt, Annette, Demarest, Keith

“…[Display omitted] A novel series of indazole/indole derivatives were discovered as glucagon receptor (GCGR) antagonists through scaffold hopping based on two…”
Get full text

Design, synthesis and biological evaluation of (2S,3R,4R,5S,6R)-5-fluoro-6-(hydroxymethyl)-2-aryltetrahydro-2H-pyran-3,4-diols as potent and orally active SGLT dual inhibitors by Xu, Guozhang, Gaul, Michael D., Kuo, Gee-Hong, Du, Fuyong, Xu, June Zhi, Wallace, Nathaniel, Hinke, Simon, Kirchner, Thomas, Silva, Jose, Huebert, Norman D., Lee, Seunghun, Murray, William, Liang, Yin, Demarest, Keith

“…[Display omitted] •A new series of SGLT1 and SGLT2 dual inhibitors were disclosed.•Two methods were developed to efficiently synthesize C5-fluoro-lactones 3…”
Get full text

Use of a Trapping Agent for Simultaneous Capturing and High-Throughput Screening of Both “Soft” and “Hard” Reactive Metabolites by Yan, Zhengyin, Maher, Noureddine, Torres, Rhoda, Huebert, Norman

“…Glutathione (GSH) has been widely used for in vitro trapping and subsequently detecting reactive metabolites using liquid chromatography−mass spectrometry. A…”
Get full text

Characterization of the ZDSD Rat: A Translational Model for the Study of Metabolic Syndrome and Type 2 Diabetes by Huebert, Norman, de Winter, Willem, Zimmerman, Karen, Jackson, Charles V., Peterson, Richard G., Hansen, Michael K.

“…Metabolic syndrome and T2D produce significant health and economic issues. Many available animal models have monogenic leptin pathway mutations that are absent…”
Get full text

Improved pharmacokinetic and bioavailability support of drug discovery using serial blood sampling in mice by Peng, Sean X, Rockafellow, Beth A, Skedzielewski, Tina M, Huebert, Norman D, Hageman, William

“…Pharmacokinetic studies in mice traditionally require one animal per time point, resulting in dosing and euthanizing a large number of animals and producing…”
Get more information

Isobaric metabolite interferences and the requirement for close examination of raw data in addition to stringent chromatographic separations in liquid chromatography/tandem mass spectrometric analysis of drugs in biological matrix by Yan, Zhengyin, Maher, Noureddine, Torres, Rhoda, Cotto, Carlos, Hastings, Becki, Dasgupta, Malini, Hyman, Rolanda, Huebert, Norman, Caldwell, Gary W.

“…In addition to matrix effects, common interferences observed in liquid chromatography/tandem mass spectrometry (LC/MS/MS) analyses can be caused by the…”
Get full text

Detection of a novel reactive metabolite of diclofenac : Evidence for CYP2C9-mediated bioactivation via arene oxides by ZHENGYIN YAN, JIAN LI, HUEBERT, Norman, CALDWELL, Gary W, YANMING DU, HUA ZHONG

“…A new glutathione adduct (M4) was tentatively identified, likely as 2'-hydroxy-3'-(glutathione-S-yl)-monoclofenac, using liquid chromatography-tandem mass…”
Get full text

Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s by Subasinghe, Nalin L., Khalil, Ehab, Travins, Jeremy M., Ali, Farah, Ballentine, Shelley K., Hufnagel, Heather R., Pan, Wenxi, Leonard, Kristi, Bone, Roger F., Soll, Richard M., Crysler, Carl S., Ninan, Nisha, Kirkpatrick, Jennifer, Kolpak, Michael X., Diloreto, Karen A., Eisennagel, Stephen H., Huebert, Norman D., Molloy, Christopher J., Tomczuk, Bruce E., Gaul, Michael D.

“…Complement C1s protease inhibitors have potential utility in the treatment of diseases associated with activation of the classical complement pathway such as…”
Get full text

FcRn binding is not sufficient for achieving systemic therapeutic levels of immunoglobulin G after oral delivery of enteric‐coated capsules in cynomolgus macaques by Muzammil, Salman, Mabus, John R., Cooper, Philip R., Brezski, Randall J., Bement, Courtney B., Perkinson, Rob, Huebert, Norman D., Thompson, Suzanne, Levine, Dalia, Kliwinski, Connie, Bradley, Dino, Hornby, Pamela J.

“…Although much speculation has surrounded intestinally expressed FcRn as a means for systemic uptake of orally administered immunoglobulin G (IgG), this has not…”
Get full text

BIOACTIVATION OF 4-METHYLPHENOL (p-CRESOL) VIA CYTOCHROME P450-MEDIATED AROMATIC OXIDATION IN HUMAN LIVER MICROSOMES by ZHENGYIN YAN, ZHONG, H. Marion, MAHER, Noureddine, TORRES, Rhoda, LEO, Gregory C, CALDWELL, Gary W, HUEBERT, Norman

“…It has previously been proposed that 4-methylphenol ( p -cresol) is metabolically activated by oxidation of the methyl group to form a reactive quinone…”
Get full text

Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif by Kreutter, Kevin D., Lu, Tianbao, Lee, Lily, Giardino, Edward C., Patel, Sharmila, Huang, Hui, Xu, Guozhang, Fitzgerald, Mark, Haertlein, Barbara J., Mohan, Venkatraman, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, McMillan, Martin, Spurlino, John C., Huebert, Norman D., Maryanoff, Bruce E., Tomczuk, Bruce E., Damiano, Bruce P., Player, Mark R.

“…2-Cyano-6-fluorophenylacetamide was explored as a novel P2 scaffold in the design of thrombin inhibitors. Optimization around this structural motif culminated…”
Get full text

Metabolism and Bioactivation of 3-Methylindole by Human Liver Microsomes by Yan, Zhengyin, Easterwood, LaHoma M, Maher, Noureddine, Torres, Rhoda, Huebert, Norman, Yost, Garold S

“…Metabolism and bioactivation of 3-methylindole (3MI) were investigated in human liver microsomes. The metabolism of two deuterium-labeled analogues of 3MI…”
Get full text

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists by Raboisson, Pierre, Marugán, Juan José, Schubert, Carsten, Koblish, Holly K., Lu, Tianbao, Zhao, Shuyuan, Player, Mark R., Maroney, Anna C., Reed, Rolanda L., Huebert, Norman D., Lattanze, Jennifer, Parks, Daniel J., Cummings, Maxwell D.

“…Novel 1,4-diazepine-2,5-diones that act as antagonists of the HDM2–p53 interaction are reported. Crystallographic analysis of ligands bound to HDM2 suggested…”
Get full text

Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors by Qiao, Lei, Baumann, Christian A., Crysler, Carl S., Ninan, Nisha S., Abad, Marta C., Spurlino, John C., DesJarlais, Renee L., Kervinen, Jukka, Neeper, Mike P., Bayoumy, Shariff S., Williams, Robyn, Deckman, Ingrid C., Dasgupta, Malini, Reed, Rolanda L., Huebert, Norman D., Tomczuk, Bruce E., Moriarty, Kevin J.

“…The discovery, SAR, and X-ray crystal structure of novel biarylaminoacyl-( S)-2-cyano-pyrrolidines and biarylaminoacylthiazolidines as potent inhibitors of…”
Get full text

Isocratic high-performance liquid chromatographic method for the separation of testosterone metabolites by Sanwald, Patricia, Blankson, Evelyn A., Duléry, Bertrand D., Schoun, Josiane, Huebert, Norman D., Dow, James

“…An isocratic reversed-phase high-performance liquid chromatographic (HPLC) method using an Ultrasphere IP column has been developed for the determination of…”
Get full text

Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes by Winters, Michael P., Sui, Zhihua, Wall, Mark, Wang, Yuanping, Gunnet, Joseph, Leonard, James, Hua, Hong, Yan, Wen, Suckow, Arthur, Bell, Austin, Clapper, Wilmelenne, Jenkinson, Celia, Haug, Peter, Koudriakova, Tatiana, Huebert, Norman, Murray, William V.

“…The discovery of a novel series of N-arylpyrroles as agonists of GPR120 (FFAR4) is discussed. Compound 27 is a potent GPR120 agonist, has good selectivity for…”
Get full text

Erratum to “Discovery of N-arylpyrroles as agonists of GPR120 for the treatment of type II diabetes” Bioorg. Med. Chem. Lett. 28 (2018) [841–846] by Winters, Michael P., Sui, Zhihua, Wall, Mark, Wang, Yuanping, Gunnet, Joseph, Leonard, James, Hua, Hong, Yan, Wen, Suckow, Arthur, Bell, Austin, Clapper, Wilmelenne, Jenkinson, Celia, Haug, Peter, Koudriakova, Tatiana, Huebert, Norman, Murray, William V.

Get full text

Enteric‐coated capsule intestinal delivery of human immunoglobulin G in cynomolgus macaques (LB603) by Mabus, John, Muzammil, Salman, Cooper, Philip, Brezski, Randall, Kunta, Jeevan, Huebert, Norman, Kliwinski, Connie, Bradley, Dino, Giles‐Komar, Jill, Hornby, Pamela

“…In adult primates, immunoglobulin G (IgG) is not detectable in the serum when taken orally due to enzymatic degradation and low intestinal permeation. Direct…”
Get full text

Pharmacokinetics of vigabatrin: implications of creatinine clearance by Haegele, K D, Huebert, N D, Ebel, M, Tell, G P, Schechter, P J

“…The pharmacokinetics of both enantiomers of vigabatrin after a single oral dose in healthy young subjects (mean creatinine clearance 120 ml/min) were compared…”
Get more information

Rapid detection and characterization of minor reactive metabolites using stable-isotope trapping in combination with tandem mass spectrometry by Yan, Zhengyin, Maher, Noureddine, Torres, Rhoda, Caldwell, Gary W., Huebert, Norman

“…Stable‐isotope trapping combined with mass spectrometry (MS) neutral loss scanning has recently been developed as a high‐throughput method for the in vitro…”
Get full text