Zobrazeno 1 - 10
of 80
pro vyhledávání: '"Ho-Sam Ahn"'
Autor:
Ho-Sam Ahn
Publikováno v:
Current Pharmaceutical Design. 9:1-2
Autor:
Ahn, Ho-Sam
Publikováno v:
Current Pharmaceutical Design; November 2003, Vol. 9 Issue: 28 pi-ii, 2p
Autor:
Stan Kurowski, Mariappan V. Chelliah, William J. Greenlee, Madhu Chintala, Yunsheng Hsieh, Yan Xia, George Boykow, Ho-Sam Ahn, Samuel Chackalamannil
Publikováno v:
ACS Medicinal Chemistry Letters. 5:183-187
We have synthesized several C7-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a from this series showed excellen
Autor:
Mariappan V. Chelliah, Tze-Ming Chan, Yan Xia, George Boykow, Madhu Chintala, Matthew Bryant, Ho-Sam Ahn, Keith Eagen, Jacqueline Agans-Fantuzzi, William J. Greenlee, Yunsheng Hsieh, Samuel Chackalamannil
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2544-2549
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey platelet aggregation assay. A potent hydroxy metab
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:
George Boykow, Samuel Chackalamannil, Andrew T. McPhail, Hsingan Tsai, William J. Greenlee, Yan Xia, Dario Doller, Ho-Sam Ahn, Michael Czarniecki, Yuguang Wang, Tze-Ming Chan, Keith Eagen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:4969-4972
The structure–activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagoinsts (e.g., 2 – 5 ) is described. The effect of the lactone carbonyl group on binding to PAR-1 is dependent on the substitution pa
Publikováno v:
Current Pharmaceutical Design. 9:2349-2365
Thrombin, a plasma serine protease, plays a key role not only in coagulation and hemostasis but in thrombosis, restenosis and atherosclerosis. Thrombin activates platelets, endothelium, inflammatory cells and smooth muscle cells. The cellular action
Publikováno v:
Current Medicinal Chemistry-Cardiovascular & Hematological Agents. 1:37-45
Protease activated receptor-1 (PAR-1), also known as thrombin receptor, is present in a variety of cell types such as platelets and endothelial cells. PAR-1 is proteolytically activated by thrombin by cleavage at its extracellular domain, unmasking a
Publikováno v:
Biochemical Pharmacology. 60:1425-1434
A growing body of evidence suggests an important contribution of the cellular actions of thrombin to thrombosis and restenosis following angioplasty. Recently we reported on SCH 79797 ( N 3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7 H -pyrrolo