Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Martin C. Clasby"'
Publikováno v:
SLAS Discovery, Vol 28, Iss 7, Pp 316-324 (2023)
Diabetes poses a global health crisis affecting individuals across age groups and backgrounds, with a prevalence estimate of 700 million people worldwide by 2045. Current therapeutic strategies primarily rely on insulin therapy or hypoglycemic agents
Externí odkaz:
https://doaj.org/article/aa92df8419fd44b28a2d2030738a26df
Autor:
Jesse W. Wotring, Sean M. McCarty, Khadija Shafiq, Charles J. Zhang, Theophilus Nguyen, Sophia R. Meyer, Reid Fursmidt, Carmen Mirabelli, Martin C. Clasby, Christiane E. Wobus, Matthew J. O’Meara, Jonathan Z. Sexton
Publikováno v:
Vaccines, Vol 10, Iss 8, p 1284 (2022)
Niclosamide, an FDA-approved oral anthelmintic drug, has broad biological activity including anticancer, antibacterial, and antiviral properties. Niclosamide has also been identified as a potent inhibitor of SARS-CoV-2 infection in vitro, generating
Externí odkaz:
https://doaj.org/article/487964f7eb2346369351c8a5aaae5f65
Autor:
Charles Lee Jayne, Santhosh Neelamkavil, Alan Hruza, Richard N. Ingram, Samuel Chackalamannil, Mariappan V. Chelliah, Keith Eagen, Teresa Andreani, William J. Greenlee, Kartik M. Keertikar, Steve Fried, Brian Hawes, Yan Xia, Zhuyan Guo, Michael P. Dwyer, Tin-Yau Chan, Paul Reichert, Martin C. Clasby
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(15)
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select comp
Autor:
Mariappan V. Chelliah, Ian W. Davies, Yan Xia, John A. Howe, Srikanth Venkatraman, Shah Unmesh G, Francisco Velazquez, Randy R. Miller, Samuel Chackalamannil, Santhosh Neelamkavil, Zhuyan Guo, Martin C. Clasby, Aileen Soriano
Publikováno v:
ACS Medicinal Chemistry Letters. 7:1173-1178
A new class of hepatitis C NS3/4A inhibitors was identified by introducing a novel spirocyclic proline–P2 surrogate onto the P2–P4 macrocyclic core of MK-5172 (grazoprevir). The potency profile of new analogues showed excellent pan-genotypic acti
Autor:
Charles Lee Jayne, Francisco Velazquez, Zhuyan Guo, Donald M. Sperbeck, Murali Rajagopalan, Duane Burnette, Karen Marcantonio, Shouwu Miao, Sathesh Bhat, Santhosh Neelamkavil, Linda Brockunier, Stacia Kargman, Yan Xia, Rebecca T. Ruck, Vincent J. Colandrea, John A. Howe, Nicole Buist, Andrew Nolting, Yongxin Han, Pinto Patrick A, Thomas Bara, Mark Cartwright, Robert Chase, Martin C. Clasby, Srikanth Venkatraman, Randy R. Miller, Keith Eagen, Samuel Chackalamannil, Josien Hubert B, Chad Bennett, Mariappan V. Chelliah, Ian W. Davies, Austin Chen, Shah Unmesh G, Sony Agrawal, Dipshikha Biswas, Jin Wu, Aileen Soriano
Publikováno v:
ACS medicinal chemistry letters. 7(1)
We have been focused on identifying a structurally different next generation inhibitor to MK-5172 (our Ns3/4a protease inhibitor currently under regulatory review), which would achieve superior pangenotypic activity with acceptable safety and pharmac
Autor:
Ho-Sam Ahn, Jacqueline Agans-Fantuzzi, Matthew Bryant, Chan Tze-Ming, George Boykow, Yan Xia, Keith Eagen, David Hesk, Madhu Chintala, Mariappan V. Chelliah, Yunsheng Hsieh, Martin C. Clasby, Xiaobang Gao, Jairam Palamanda, William J. Greenlee, Samuel Chackalamannil
Publikováno v:
Journal of Medicinal Chemistry. 50:5147-5160
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort has resulted in the identification of seve
Autor:
Keith Eagen, Andrew T. McPhail, William J. Greenlee, Yunsheng Hsieh, Madhu Chintala, Samuel Chackalamannil, Yan Lin, Hsingan Tsai, Jayaram R. Tagat, Dario Doller, Ho-Sam Ahn, Yan Xia, George Boykow, Martin C. Clasby, Jacqueline Agans-Fantuzzi, Michael Czarniecki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3647-3651
The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent compound 40 had an IC(50) of 7.6 nM and showed robust inhib
Autor:
Keith Eagen, Dario Doller, Martin C. Clasby, Andrew T. McPhail, Hsingan Tsai, Yan Xia, Yan Lin, Samuel Chackalamannil
Publikováno v:
Tetrahedron Letters. 41:4043-4047
An efficient, multigram-scale synthesis of dihydronaphthofuranone 1 using a novel aryl intramolecular Diels–Alder reaction of propargyl trans -cinnamate 8 is described. Catalytic reduction of 1 gave the cis -fused tetrahydronaphthofuranone derivati
Autor:
Justine Yeun Quai Lai, Albert A. Jaxa-Chamiec, Martin C. Clasby, Andrew J. P. White, Alexandra M. Z. Slawin, Andrew Marsh, Donald Craig, David J. Williams
Publikováno v:
Tetrahedron. 52:4769-4802
The enantiospecific synthesis of the vitamin D3 CD ring fragment 3 is reported. Key steps are the diastereoselective allylation of a norephedrine/dihydrocitronellic acid-derived oxazolidinone, and the intramolecular Diels-Alder reaction of a sulfonyl
Publikováno v:
Synlett. 1995:467-474