Zobrazeno 1 - 10
of 10
pro vyhledávání: '"Russell J. DeOrazio"'
Autor:
Andrew J. Mhyre, Cheng Guo, Russell J. DeOrazio, Kevin Fitzpatrick, Yuri L. Khmelnitsky, Zhenjun Zhang, Min Hu, Peter R. Guzzo, Susan Tom, Jun-Ho Maeng, Douglas B. Kitchen, Michele Luche, Shuang Liu, Alexander Usyatinsky
Publikováno v:
Bioorganic & Medicinal Chemistry. 22:3414-3422
The sodium glucose co-transporter 2 (SGLT2) has received considerable attention in recent years as a target for the treatment of type 2 diabetes mellitus. This report describes the design, synthesis and structure-activity relationship (SAR) of C-glyc
Autor:
Sham S. Nikam, Russell J. DeOrazio, David D. Manning, Scott Ian L, Brian Alan Sherer, Jun-Ho Maeng
Publikováno v:
Synthetic Communications. 41:3551-3555
The double metallation of 6-bromo-3H-benzothiazol-2-one and 6-bromo-3H-benzoxazol-2-one with methyl magnesium bromide and alkyllithium bases is described. Alkylation with a variety of electrophiles occurs at the 6-position of the heterocycles in good
Autor:
Timothy Rust, Carla Hassler, James P. Harding, Justin J. Richards, Brian I. Bliss, Yuri L. Khmelnitsky, David D. Manning, Marlene L. Cohen, Liaqat Masih, Michael A. Lynch, Jianqing Chen, Kevin L. Christensen, Zhicai Yang, Soshanna Isaacson, Jonathan D. Wierschke, Cathy M. Beer, Russell J. DeOrazio, Jun-Ho Maeng, Lisa H. Peterson, Christopher L. Cioffi, Alexander Usyatinsky, Kevin Fitzpatrick, David J. Fairfax, Matthew Isherwood, Svetlana Dobritsa, W. Martin Rennells
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6538-6541
A new class of 2-substituted benzoxazole carboxamides are presented as potent functional 5-HT(3) receptor antagonists. The chemical series possesses nanomolar in vitro activity against human 5-HT(3)A receptors. A chemistry optimization program was co
Autor:
Douglas B. Kitchen, Svetlana Dobritsa, Mei Bai, Thomas D. Friedrich, Peter R. Guzzo, Grant J. Carr, Mark A. Wolf, Michael A. Lynch, Alexander Usyatinsky, Russell J. DeOrazio, Denise Peace, Kevin Fitzpatrick, Mohammed Sajad
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3017-3020
An indazole based series of glucocorticoid receptor agonists is reported. The SAR exploration of this scaffold yielded compounds with nanomolar affinity for the glucocorticoid receptor with indications of selectivity for the preferred transrepression
Autor:
Brian Nichelson, Mark G. Vartanian, Charles Taylor, Susan M. Lotarski, Nancy Sue Barta, Sean D. Donevan, Sian E. Gibbons, Norman L. Colbry, Zhu Zhijian, Melvin R. Dickerson, Paul Galatsis, Russell J. DeOrazio, Jacob Bradley Schwarz, Kristin Knapp Lin, Zheng Li, Andrew John Thorpe, Jack J. Kinsora, Raymond Andrew Hudack, David J. Wustrow, David D. Manning, Ayman El-Kattan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3559-3563
Several beta-amino tetrazole analogs of gabapentin 1 and pregabalin 2 were prepared by one of two convergent, highly efficient routes, and their affinity for the alpha(2)-delta protein examined. Two select compounds with potent affinity for alpha(2)-
Publikováno v:
Synthetic Communications. 35:979-985
An impurity isolated during the kilo‐lab preparation of 3β‐acetoxyandrost‐5‐ene‐7,17‐dione was identified as 3β‐acetoxy‐17a‐oxo‐androst‐5‐ene‐7,17‐dione. This novel D‐ring secosteroid was postulated to be a Baeyer–Vi
Autor:
Alicia J Habershaw, Bernard Paul, Mark A Helle, David C Burdick, Peter R. Guzzo, Russell J. DeOrazio, Mark A. Wolf
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1424-1426
A novel series of Delta9-tetrahydrocannabinol (Delta9-THC) analogues were synthesized to determine their potential as cannabinoid receptor modulators. Chemistry focused on conversion of the phenol of Delta9-THC to other functionality through palladiu
Publikováno v:
Carbohydrate Research. 317:210-216
The stereospecific formation of α- d -mannosyl glycosidic linkages has been achieved in high yield using tetra- O -pivaloyl-α- d -mannopyranosyl fluoride and boron trifluoride diethyl etherate in dichloromethane. Examples of the α- d -mannosylatio
Autor:
Russell J. DeOrazio, Scott Ian L, David D. Manning, Jun-Ho Maeng, Brian Alan Sherer, Sham S. Nikam
Publikováno v:
ChemInform. 43
The double metallation of 6-bromo-3H-benzothiazol-2-one and 6-bromo-3H-benzoxazol-2-one with methyl magnesium bromide and alkyllithium bases is described. Alkylation with a variety of electrophiles occurs at the 6-position of the heterocycles in good
Publikováno v:
ChemInform. 30
The stereospecific formation of α- d -mannosyl glycosidic linkages has been achieved in high yield using tetra- O -pivaloyl-α- d -mannopyranosyl fluoride and boron trifluoride diethyl etherate in dichloromethane. Examples of the α- d -mannosylatio