Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Mariappan V. Chelliah"'
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:
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:
Christopher Joseph Sinz, Sarah Souza, Aimie M. Ogawa, Dennis Leung, Eric R. Ashley, Brande Thomas-Fowlkes, Maria Madeira, Mary Ann Powles, Effie Tozzo, Hong D. Chu, Feroze Ujjainwalla, Melissa Kirkland, Matthew Lombardo, Clare London, Jerry Di Salvo, Keith Eagen, John S. Debenham, Jason M. Cox, Ping Lan, Alejandro Crespo, Adam B. Weinglass, Taro E. Akiyama, Nengxue Wang, Henry M. Vaccaro, Michele Pachanski, Shah Unmesh G, Zhongxiang Sun, Mariappan V. Chelliah, James R. Tata, Michael A. Plotkin, Candice Alleyne, Takao Suzuki, Srikanth Venkatraman
Publikováno v:
ACS medicinal chemistry letters. 8(1)
Type 2 diabetes mellitus (T2DM) is an ever increasing worldwide epidemic, and the identification of safe and effective insulin sensitizers, absent of weight gain, has been a long-standing goal of diabetes research. G-protein coupled receptor 120 (GPR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28a251742e59339ae232f1fad2130722
https://pubmed.ncbi.nlm.nih.gov/28105274
https://pubmed.ncbi.nlm.nih.gov/28105274
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
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59cc61ee2f05b48391d822d3acecca21
https://doi.org/10.1021/jm070704k
https://doi.org/10.1021/jm070704k
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c7e00f3c3f4a58b31fcc5937b720a0e8
https://pubmed.ncbi.nlm.nih.gov/26819676
https://pubmed.ncbi.nlm.nih.gov/26819676
Publikováno v:
The Journal of Organic Chemistry. 63:3087-3098
Areneruthenium chemistry was used to effect intramolecular SNAr reactions between phenoxide nucleophiles and chlorophenylalanine residues that are connected by a peptide chain, resulting in the construction of a bicyclic peptido aryl ether system tha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7b7e32ce681908e67a2422e790dca6fa
https://doi.org/10.1021/jo980060b
https://doi.org/10.1021/jo980060b