Zobrazeno 1 - 10
of 106
pro vyhledávání: '"Samuel Chackalamannil"'
Autor:
Samuel Chackalamannil
Publikováno v:
Medicinal Chemistry Research. 31:1623-1636
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e3065a3f0a362231c651329093b30272
https://doi.org/10.1007/s00044-022-02938-3
https://doi.org/10.1007/s00044-022-02938-3
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c095f071ef48433855bcea54d91788f5
https://pubmed.ncbi.nlm.nih.gov/32527459
https://pubmed.ncbi.nlm.nih.gov/32527459
Autor:
Charles Lee Jayne, Hong Liu, Yan Xia, Santhosh Neelamkavil, William J. Greenlee, Hana Baker, Brian Hawes, Kim O’Neill, Andrew Stamford, Timothy J. Kowalski, Xing Dai, Jinsong Hao, Samuel Chackalamannil, Huadong Tang, Dipshikha Biswas, Bernard R. Neustadt, Craig D. Boyle
Publikováno v:
ACS Medicinal Chemistry Letters. 9:457-461
[Image: see text] The ever-growing prevalence of type 2 diabetes in the world has necessitated an urgent need for multiple orally effective agents that can regulate glucose homeostasis with a concurrent reduction in body weight. G-Protein coupled rec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ccb59bda5cd880fcaccd1cfaabd07b78
https://doi.org/10.1021/acsmedchemlett.8b00073
https://doi.org/10.1021/acsmedchemlett.8b00073
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f17e337afff84cf9a865c88293e12d7
https://doi.org/10.1021/acsmedchemlett.6b00321
https://doi.org/10.1021/acsmedchemlett.6b00321
Publikováno v:
Lead Generation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c27c782d3362f785bde05a524fbb0f5a
https://doi.org/10.1002/9783527677047.ch19
https://doi.org/10.1002/9783527677047.ch19
Autor:
Keith Eagen, Yunsheng Hsieh, Mariappan V. Chelliah, Stan Kurowski, Zhuyan Guo, Madhu Chintala, William J. Greenlee, Hsingan Tsai, Samuel Chackalamannil, Ho-Sam Ahn, Yan Xia, George Boykow
Publikováno v:
ACS Medicinal Chemistry Letters. 5:561-565
We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar. Compound 5c from this series sh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5167ac4b35159c9670df81e0eaf948e6
https://doi.org/10.1021/ml500008w
https://doi.org/10.1021/ml500008w
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64b51fb9c036df9fa0fa9ec39ff0de40
https://doi.org/10.1021/ml400452v
https://doi.org/10.1021/ml400452v
Autor:
Samuel Chackalamannil
Publikováno v:
Medicinal Chemistry Reviews ISBN: 9780996293235
Medicinal Chemistry Reviews
Medicinal Chemistry Reviews
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7ff66f866b000bbe887307eba5bbb85f
https://doi.org/10.29200/acsmedchemrev-v51.ch23
https://doi.org/10.29200/acsmedchemrev-v51.ch23
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e94036f493fa5d675af5fc8cc2d8746b
https://doi.org/10.1016/j.bmcl.2012.01.138
https://doi.org/10.1016/j.bmcl.2012.01.138