Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Natasha M. Kablaoui"'
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:415-419
Oxytocin (OT) is a peptide hormone agonist of the oxytocin receptor (OTR) that has been proposed as a therapeutic to treat a number of social and emotional disorders in addition to its current clinical use to induce labor and treat postpartum bleedin
Autor:
Christopher Ryan Butler, Qingyi Yang, Michael Popiolek, Natasha M. Kablaoui, Lei Zhang, Sarah Grimwood, John T. Lazzaro, Rouba Kozak, Damien Webb, Rebecca E. O’Connor, Erik Alphie Lachapelle
Publikováno v:
ACS Med Chem Lett
[Image: see text] It has been hypothesized that selective muscarinic acetylcholine receptor (mAChR) M4 subtype activation could provide therapeutic benefits to a number of neurological disorders while minimizing unwanted cholinergic side effects obse
Autor:
Bruce N. Rogers, Simone Sciabola, Kari R. Fonseca, Natasha M. Kablaoui, David Gray, Michelle Vanase-Frawley, Guoyun Bai, Gilles H. Goetz, Allen J. Duplantier
Publikováno v:
Bioorganic & Medicinal Chemistry. 24:3513-3520
Oxytocin (OT) is a peptide hormone agonist of the OT receptor (OTR) that plays an important role in social behaviors such as pair bonding, maternal bonding and trust. The pharmaceutical development of OT as an oral peptide therapeutic has been hinder
Autor:
Francioise Berlioz, Michael L. Vazquez, Natasha M. Kablaoui, Keith Hoffmaster, Douglas Demian, Richard A. Nugent, Snahel Patel, William M. Moore, Jay Shao
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:907-911
A novel series of potent benzoxazole mPGES-1 inhibitors has been derived from a hit from a high throughput screen. Compound 37 displays mPGES-1 inhibition in an enzyme assay (0.018 μM) and PGE-2 inhibition in a cell-based assay (0.034 μM). It demon
Autor:
Daniel P. Walker, Alexander F. Shaffer, William M. Moore, Michael T. Baratta, Sue Metz, Jeffrey A. Scholten, John Robert Springer, Jeffrey S. Carter, Hwang-Fun Lu, Steven E. Heasley, Yvette M. Fobian, Natasha M. Kablaoui, Francisco M. Franco, Li Xing, Shengtian Yang, Hanau Cathleen E, Michael L. Vazquez, Graciela B. Arhancet, Gina M. Jerome
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1120-1126
Microsomal prostaglandin E(2) synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed the discovery of clinical candidate PF-04693627, a potent mPGES-1 inhibitor possessing a
Autor:
Eric Feyfant, Natasha M. Kablaoui, Heather McInnes, Sarah M. Osgood, Michelle Vanase-Frawley, Ramin Darvari, Angela C. Doran, Kari R. Fonseca, Derek L. Buhl, Mark J. Majchrzak, Meera E. Modi
Publikováno v:
The Journal of Pharmacology and Experimental Therapeutics
Oxytocin (OT) modulates the expression of social and emotional behaviors and consequently has been proposed as a pharmacologic treatment of psychiatric diseases, including autism spectrum disorders and schizophrenia; however, endogenous OT has a shor
Autor:
Hu Liu, Cyrille Kuhn, Rahul Sharma, Natasha M. Kablaoui, Gordon Alton, Miret Juan, Brendan Connolly, Robert V. Stanton, Ping Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:849-852
S6K1 (p70 S6 kinase-1) is thought to play a critical role in the development of obesity and insulin resistance, thus making it an attractive target in developing medicines for the treatment of these disorders. We describe a novel thiophene urea class
Autor:
Archana Chaudhry, Gary Bora, Robin Roof, Jiansu Zhang, Natasha M. Kablaoui, Maura E. Charlton, Bradley Snyder, Wendy M. Habeski, Cheryl Li, Snahel Patel, Hyunsuk Min, Brian M. Campbell, Douglas S. Johnson, Debra Hidayetoglu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5689-5693
The discovery of the CNS-penetrant and selective α 2C adrenergic receptor antagonist N -{2-[4-(2,3-dihydro-benzo[1,4]dioxin-2-ylmethyl)-[1,4]diazepan-1-yl]-ethyl}-2-phenoxy-nicotinamide, 13 is described. Structure–activity studies demonstrate the
Publikováno v:
Journal of the American Chemical Society. 121:5881-5898
A Pauson−Khand type conversion of enynes to bicyclic cyclopentenones employing the commercially available precatalyst titanocene dicarbonyl is described. This methodology shows excellent functional group tolerance for a group 4 metallocene-catalyze
Publikováno v:
Journal of the American Chemical Society. 119:4424-4431
A method for the transformation of o-allyl aryl ketones to γ-butyrolactones using a catalytic amount of Cp2Ti(PMe3)2 or Cp2Ti(CO)2 is described. This catalytic “hetero Pauson−Khand”-type process proceeds via the carbonylation of an oxatitanacy