Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Bireshwar Dasgupta"'
Autor:
Richard A. Hartz, Vijay T. Ahuja, Susheel J. Nara, C. M. Vijaya Kumar, Raju K. V. L. P. Manepalli, Sarat Kumar Sarvasiddhi, Swarnamba Honkhambe, Vidya Patankar, Bireshwar Dasgupta, Ramkumar Rajamani, Jodi K. Muckelbauer, Daniel M. Camac, Kaushik Ghosh, Matthew Pokross, Susan E. Kiefer, Jeffrey M. Brown, Lisa Hunihan, Michael Gulianello, Martin Lewis, Jonathan S. Lippy, Neha Surti, Brian D. Hamman, Jason Allen, Walter A. Kostich, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba
Publikováno v:
Journal of Medicinal Chemistry. 65:4121-4155
Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of neuropathic pain. Inhibition of AAK1 in the central nervous system, particularly within the spinal co
Autor:
Zhi Liang, Alan Wilson, Li Dong, Neil T. Burford, David S. Kimball, Kenneth G. Carson, Yingzhi Bi, Yulian Zhang, Bireshwar Dasgupta, Carolyn Diane Dzierba, Richard A. Hartz, James E. Grace, G. Greg Zipp, Soojin Kwon, Martin A. Lewis, Joanne J. Bronson, Cynthia Anne Fink, Amr Nouraldeen, Saadat Aleem, Giovanni Cianchetta, Jiancheng Wang, Ying Liu, Vijay T. Ahuja, Robert L. Bertekap, Jianxin Han, Michael Alan Green, Angela Cacace, Godwin Kumi, Yudith Garcia, Ying Qiao, Meredith Ferrante, John E. Macor, Ryan Westphal
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:1448-1452
Small molecule modulators of GPR88 activity (agonists, antagonists, or modulators) are of interest as potential agents for the treatment of a variety of psychiatric disorders including schizophrenia. A series of phenylglycinol and phenylamine analogs
Autor:
Daniel R. Schroeder, Vivekananda M. Vrudhula, Charlie M. Conway, Cen Xu, Gene M. Dubowchik, Bireshwar Dasgupta, John E. Macor, Sokhom S. Pin, Edward S. Kozlowski, John R. Torrente
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:2744-2748
An oxidation product (5) formed during the synthesis of BIBN-4096BS (1) was found to be a potent CGRP antagonist (IC50 = 0.11 nM). While 5 was found to be ten-fold less potent than 1, another analog 8 with lower molecular weight containing the oxidiz
Autor:
Bang-Chi Chen, Vijay T. Ahuja, Daniel Smith, Subramaniam Krishnananthan, Joanne J. Bronson, Bireshwar Dasgupta, Jianqing Li, Richard A. Hartz, William D. Schmitz, Joel C. Barrish, Arvind Mathur
Publikováno v:
Organic Process Research & Development. 16:156-159
An efficient scale-up synthesis of (S)-5-chloro-1-(1-cyclopropylethyl)-3-(2,6-dichloro-4-(difluoromethoxy)phenylamino)-pyrazin-2(1H)-one, 1 (BMS-665053), is described. This new process features a one-step direct bis-ortho-chlorination of 4-(difluorom
Autor:
Gene M. Dubowchik, Kaitlin E. Browman, Lynn A. Balanda, Kevin D. Burris, John E. Macor, Bireshwar Dasgupta, Sokhom S. Pin, Vivekananda M. Vrudhula, Lawrence K. Fung, Matthew T. Taber, Tracey Fiedler, Jie Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1905-1909
Several tetrahydroimidazopyrimidines were prepared using silver assisted cyclization as the key step. The binding affinities of compounds thus prepared were evaluated in vitro toward hCRF(1)R. Initial lead compound 16 (K(i)=32 nM) demonstrated modest
Autor:
Gene M. Dubowchik, Karin Sipman, Vivekananda M. Vrudhula, Todd A. Verdoorn, Alexander Vinitsky, Bireshwar Dasgupta, Sagarika Bollini, Ti Chen, Steven Sheriff, Jeffrey Tredup, Dolatrai M. Vyas, Jonathan L. Ditta, Mark R. Witmer
Publikováno v:
Organic Letters. 3:3987-3990
[structure: see text] 2-Aryl-2,2-difluoroacetamido-proline and pipecolate esters are high affinity FKBP12 ligands whose rotamase inhibitory activity is comparable to that seen for the corresponding ketoamides. X-ray structural studies suggest that th
Publikováno v:
Tetrahedron: Asymmetry. 9:3781-3788
The enantioselective preparation of 2-(3′ R ,5′ R -diacetoxy-6 E ,8 E -decadienyl)-1,3-dioxane, (+)- 13 , is described. This synthesis of the skeleton of streptenol D utilizes the ability of a diene-complexed (tricarbonyl)iron unit to serve as a
Publikováno v:
Tetrahedron Letters. 39:343-346
The oxidation of (dienol)iron complexes to the corresponding (dienal)iron complexes by amine N-oxides is reported. This oxidation is selective for a hydroxyl group adjacent to the complexed diene.
Autor:
Huameng Li, Bireshwar Dasgupta, Richard A. Craig, Rodger Henry, William A. Donaldson, James Thomas Wasicak
Publikováno v:
Tetrahedron. 53:4185-4198
The alkylation of (4,6-heptadien-3-one)- and (methyl 3,5-hexadienoate)Fe(CO) 3 ( 1 and 2 ) were examined (0–42% de and 69–92% de respectively). Optically active (methyl 3,5-hexadienoate)Fe(CO) 3 (−)- 2 was prepared by resolution of the correspo
Autor:
Maria Rafalski, Thais M. Sielecki, Bireshwar Dasgupta, Paul J. Gilligan, Padmaja Kasireddy-Polam, Thaddeus F. Molski, Argyrios G. Arvanitis, Nicholas J. Lodge, John E. Macor, Andrew P. Combs, Amy Galka, Shikha Vig, Amy G. Takvorian, Harvey Wong, George L. Trainor, Tricia L. Johnson, Carolyn Diane Dzierba, Joanne J. Bronson, Ge Zhang, Robert Zaczek
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(15)
Pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones were evaluated as corticotropin-releasing factor-1 receptor antagonists. The synthesis, SAR studies and pharmacokinetic evaluation of these analogs are described herein.