Search Results - "ALBERT, Jeffrey S"

Pharmacological property optimization for allosteric ligands: A medicinal chemistry perspective by Johnstone, Shawn, Albert, Jeffrey S.

“…[Display omitted] New strategies to potentially improve drug safety and efficacy emerge with allosteric programs. Biased allosteric modulators can be designed…”
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Multiple roles of transient receptor potential (TRP) channels in inflammatory conditions and current status of drug development by Radresa, Olivier, Paré, Michel, Albert, Jeffrey S

“…During inflammation, several Transient Receptor Potential (TRP) channels are directly or indirectly activated by inflammatory signaling molecules and…”
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Efficient synthesis of a 7-azabicyclo[2.2.1]heptane based GlyT1 uptake inhibitor by Xiong, Hui, Frietze, William, Andisik, Donald W., Ernst, Glen E., Palmer, William E., Hinkley, Lindsay, Varnes, Jeffrey G., Albert, Jeffrey S., Veale, Chris A.

“…Generation and subsequent electrophilic reaction of a Boc-protected azabicyclo[2.2.1]heptane anion led to efficient preparation of the potent GlyT1 uptake…”
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Asymmetric Synthesis of a Potent CXCR7 Modulator Featuring a Hindered Tertiary β‑Amino Amide Stereocenter by Canterbury, Daniel P, Godin, Francois, Desjardins, Samuel, Bayrakdarian, Malken, Albert, Jeffrey S, Perry, David A, Hesp, Kevin D

“…A practical and asymmetric synthesis of a small-molecule CXCR7 modulator featuring a highly functionalized and hindered tertiary β-amino amide framework is…”
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Application of Fragment-Based Lead Generation to the Discovery of Novel, Cyclic Amidine β-Secretase Inhibitors with Nanomolar Potency, Cellular Activity, and High Ligand Efficiency by Edwards, Philip D, Albert, Jeffrey S, Sylvester, Mark, Aharony, David, Andisik, Donald, Callaghan, Owen, Campbell, James B, Carr, Robin A, Chessari, Gianni, Congreve, Miles, Frederickson, Martyn, Folmer, Rutger H. A, Geschwindner, Stefan, Koether, Gerard, Kolmodin, Karin, Krumrine, Jennifer, Mauger, Russell C, Murray, Christopher W, Olsson, Lise-Lotte, Patel, Sahil, Spear, Nate, Tian, Gaochao

“…Fragment-based lead generation has led to the discovery of a novel series of cyclic amidine-based inhibitors of β-secretase (BACE-1). Initial fragment hits…”
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Design, Synthesis, and SAR of Tachykinin Antagonists:  Modulation of Balance in NK1/NK2 Receptor Antagonist Activity by Albert, Jeffrey S, Aharony, David, Andisik, Donald, Barthlow, Herbert, Bernstein, Peter R, Bialecki, Russell A, Dedinas, Robert, Dembofsky, Bruce T, Hill, Daniel, Kirkland, Karin, Koether, Gerard M, Kosmider, Benedict J, Ohnmacht, Cyrus, Palmer, William, Potts, William, Rumsey, William, Shen, Lihong, Shenvi, Ashok, Sherwood, Scott, Warwick, Paul J, Russell, Keith

“…Through optimization of compounds based on the dual NK1/NK2 antagonist ZD6021, it was found that alteration of two key regions could modulate the balance of…”
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Discovery of a Novel Warhead against β-Secretase through Fragment-Based Lead Generation by Geschwindner, Stefan, Olsson, Lise-Lotte, Albert, Jeffrey S, Deinum, Johanna, Edwards, Philip D, de Beer, Tonny, Folmer, Rutger H. A

“…Fragment-based lead generation was applied to find novel small-molecule inhibitors of β-secretase (BACE-1), a key target for the treatment of Alzheimer's…”
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Development of a Plate-Based Optical Biosensor Fragment Screening Methodology to Identify Phosphodiesterase 10A Inhibitors by Geschwindner, Stefan, Dekker, Niek, Horsefield, Rob, Tigerström, Anna, Johansson, Patrik, Scott, Clay W, Albert, Jeffrey S

“…We describe the development of a novel fragment screening methodology employing a plate-based optical biosensor system that can operate in a 384-well format…”
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Structural Analysis and Optimization of NK1 Receptor Antagonists through Modulation of Atropisomer Interconversion Properties by Albert, Jeffrey S, Ohnmacht, Cyrus, Bernstein, Peter R, Rumsey, William L, Aharony, David, Alelyunas, Yun, Russell, Daniel J, Potts, William, Sherwood, Scott A, Shen, Lihong, Dedinas, Robert F, Palmer, William E, Russell, Keith

“…We have previously described a series of antagonists that showed high potency and selectivity for the NK1 receptor. However, these compounds also had the…”
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Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists by Laliberté, Sébastien, Vallée, Frédéric, Fournier, Pierre-André, Bedard, Leanne, Labrecque, Jean, Albert, Jeffrey S.

“…We describe the discovery and advancement of a novel series of TRPA1 antagonist having an aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamide scaffold…”
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Naphtho[2,1-b][1,5] and [1,2-f][1,4]oxazocines as selective NK1 antagonists by OHNMACHT, Cyrus J, ALBERT, Jeffrey S, BERNSTEIN, Peter R, RUMSEY, William L, MASEK, Brian B, DEMBOFSKY, Bruce T, KOETHER, Gerard M, ANDISIK, Donald W, AHARONY, David

“…Previously we reported on the synthesis and properties of a series of highly potent piperidinyl 2-subsituted-3-cyano-1-naphthamide NK1 antagonists that…”
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Stabilization of Helical Domains in Short Peptides Using Hydrophobic Interactions by Albert, Jeffrey S, Hamilton, Andrew D

“…The contribution of hydrophobic interactions in the stabilization of helical structure was compared for a series of short peptides that incorporated two…”
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Molecular Recognition of Proteins: Sequence-Selective Binding of Aspartate Pairs in Helical Peptides by Albert, Jeffrey S, Goodman, M. Scott, Hamilton, Andrew D

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Bicyclo((aryl)methyl)benzamides as inhibitors of GlyT1 by Varnes, Jeffrey G., Xiong, Hui, Forst, Janet M., Holmquist, Christopher R., Ernst, Glen E., Frietze, William, Dembofsky, Bruce, Andisik, Don W., Palmer, William E., Hinkley, Lindsay, Steelman, Gary B., Wilkins, Deidre E., Tian, Gaochao, Jonak, Gerald, Potts, William M., Wang, Xia, Brugel, Todd A., Alhambra, Cristóbal, Wood, Michael W., Veale, Chris A., Albert, Jeffrey S.

“…A series of isoquinuclidines and bicyclic analogs were investigated as inhibitors of glycine uptake for the treatment of schizophrenia. Dimethylbenzamide 9…”
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Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists by Hu, Yun-Jin, St.-Onge, Miguel, Laliberté, Sébastien, Vallée, Frédéric, Jin, Shujuan, Bedard, Leanne, Labrecque, Jean, Albert, Jeffrey S.

“…A series of TRPA1 antagonists is described having a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine or a 1-aryloxyisoquinoline scaffold. These compounds have high ligand…”
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Fragment-assisted hit investigation involving integrated HTS and fragment screening: Application to the identification of phosphodiesterase 10A (PDE10A) inhibitors by Varnes, Jeffrey G., Geschwindner, Stefan, Holmquist, Christopher R., Forst, Janet, Wang, Xia, Dekker, Niek, Scott, Clay W., Tian, Gaochao, Wood, Michael W., Albert, Jeffrey S.

“…[Display omitted] Fragment-based drug design (FBDD) relies on direct elaboration of fragment hits and typically requires high resolution structural information…”
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Discovery of a Novel Muscarinic Receptor PET Radioligand with Rapid Kinetics in the Monkey Brain by Malmquist, Jonas, Varnäs, Katarina, Svedberg, Marie, Vallée, Frédéric, Albert, Jeffrey S, Finnema, Sjoerd J, Schou, Magnus

“…Positron emission tomography (PET), together with a suitable radioligand, is one of the more prominent methods for measuring changes in synaptic…”
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Discovery of novel, orally active dual NK1/NK2 antagonists by BERNSTEIN, Peter R, AHARONY, David, KOSMIDER, Benedict J, KIRKLAND, Karin, OHNMACHT, Cyrus J, POTTS, William, RUMSEY, William L, LIHONG SHEN, SHENVI, Ashok, SHERWOOD, Scott, STOLLMAN, David, RUSSELL, Keith, ALBERT, Jeffrey S, ANDISIK, Donald, BARTHLOW, Herbert G, BIALECKI, Russell, DAVENPORT, Timothy, DEDINAS, Robert F, DEMBOFSKY, Bruce T, KOETHER, Gerard

“…Exploration of the SAR around selective NK2 antagonists, SR48968 and ZD7944, led to the discovery that naphth-1-amide analogues provide potent dual NK1 and NK2…”
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An integrated approach to fragment-based lead generation: philosophy, strategy and case studies from AstraZeneca's drug discovery programmes by Albert, Jeffrey S, Blomberg, Niklas, Breeze, Alexander L, Brown, Alastair J H, Burrows, Jeremy N, Edwards, Philip D, Folmer, Rutger H A, Geschwindner, Stefan, Griffen, Ed J, Kenny, Peter W, Nowak, Thorsten, Olsson, Lise-Lotte, Sanganee, Hitesh, Shapiro, Adam B

“…Fragment-based lead generation (FBLG) has recently emerged as an alternative to traditional high throughput screening (HTS) to identify initial chemistry…”
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Progress in the development of beta-secretase inhibitors for Alzheimer's disease by Albert, Jeffrey S

“…Since the original identification of BACE in 1999 and until quite recently, BACE was often regarded as a "difficult" drug target, much as renin has proven to…”
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