Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Liangqin Guo"'
Autor:
Nicolas Solban, Alexander Pasternak, Qinglin Pu, Amy C. Doty, David Jonathan Bennett, Charles A. Lesburg, Wensheng Yu, Prasanthi Geda, Nunzio Sciammetta, J. Richard Miller, Hua Zhou, Xuelei Song, Yongxin Han, Lars Neumann, David L. Sloman, Mangeng Cheng, Heidi Ferguson, Karin M. Otte, Liangqin Guo, Hongjun Zhang, Alfred Lammens, Xavier Fradera, Meredeth A. McGowan
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine-2,3-dioxygenase 1 (IDO1) inhibition and its combination with immune checkpoint inhibitors like pembrolizumab have drawn considerable attention from both academia and the pharmaceutical industry. Here, we describe the dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bc457a333eeebf89280777405619540
https://doi.org/10.1021/acsmedchemlett.0c00195
https://doi.org/10.1021/acsmedchemlett.0c00195
Autor:
Harold B. Wood, Kunal Desai, Daming Feng, Jamie McCabe-Dunn, Yi-Heng Chen, Edward C. Sherer, Jane Y. Wu, Marc Poirier, Hong Li, Dongfang Meng, Ting Zhang, Kenneth P. Ellsworth, Liangqin Guo, Teruyuki Nishimura, Jiayi Xu, Tomokazu Hirabayashi, Sunita V. Dewnani, Patrick Andre, Louis-Charles Campeau, Richard Tschirret-Guth, Isao Sakurada, Paul Reichert, Cameron J. Smith, Robert K. Orr, Lisa M. Sonatore, Wayne M. Geissler, Thomas Bateman, Kazuto Araki, Joe Metzger, Alan Hruza, Richard A. Berger, Dann L. Parker, Tianying Jian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:5437-5443
Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High selectivity over FXa inhibition was achieved. Selected compounds were evaluated in rat IV/PO pharmacokinetic (PK) s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ff96f55b80c75cf4042ca06570740e9
https://doi.org/10.1016/j.bmcl.2015.07.078
https://doi.org/10.1016/j.bmcl.2015.07.078
Autor:
Donald Nelson, Gary G. Chicchi, James Dellureficio, Ravi P. Nargund, Peter H. Dobbelaar, Liangqin Guo, Kwei-Lan Tsao, Janet S. Kerr, Bei Zhang, Zhong Lai, Patricia R. Bunting, Shrenik K. Shah, Raman K. Bakshi, Qingmei Hong, Hongbo Qi, Guillermo Fernandez, Mikhail Reibarkh, Qing Shao, Quang Truong, Koppara Samuel, Jian Liu, Sylvia Volksdorf, Zhixiong Ye, Yun-Ping Zhou, Margaret Wu, Cai Li, Stan Mitelman, Andrew D. Howard, Wu Du, Maria E. Trujillo, George J. Eiermann, Shuwen He, Vijay Bhasker G. Reddy, Tianying Jian, Pierre Morissette, Patrick Fitzgerald, Dorina Trusca, Sharon Tong, William K. Hagmann
Publikováno v:
ACS Medicinal Chemistry Letters. 5:748-753
Antagonism of somatostatin subtype receptor 3 (sstr3) has emerged as a potential treatment of Type 2 diabetes. Unfortunately, the development of our first preclinical candidate, MK-4256, was discontinued due to a dose-dependent QTc (QT interval corre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ced576c72131916fe1527dabb0d36e73
https://doi.org/10.1021/ml500028c
https://doi.org/10.1021/ml500028c
Autor:
Qinglin Pu, Hongjun Zhang, Liangqin Guo, Mangeng Cheng, Doty, Amy C., Ferguson, Heidi, Fradera, Xavier, Lesburg, Charles A., McGowan, Meredeth A., Miller, J. Richard, Geda, Prasanthi, Xuelei Song, Otte, Karin, Nunzio Sciammetta, Solban, Nicolas, Wensheng Yu, Sloman, David L., Hua Zhou, Lammens, Alfred, Neumann, Lars
Publikováno v:
ACS Medicinal Chemistry Letters; 8/13/2020, Vol. 11 Issue 8, p1548-1554, 7p
Autor:
John S. Debenham, Dann L. Parker, Birgit T. Priest, Ravi P. Nargund, Feroze Ujjainwalla, Randal M. Bugianesi, Michele Pachanski, Liangqin Guo, William K. Hagmann, George J. Eiermann, Yi Zang, Ramzi F. Sweis, Andrew D. Howard, Jenna L. Terebetski, Melissa Kirkland, Yue Feng, Gino Salituro, Derun Li, Christopher Joseph Sinz, Stan Mitelman, Maria E. Trujillo, Scott D. Edmondson, Karen H. Dingley, Jin Shang, Nicole Buist, Xiaofang Li, Weiguo Liu, Mary Ann Powles, Terri M. Kelly, Edward C. Sherer
GPR142 has been identified as a potential glucose-stimulated insulin secretion (GSIS) target for the treatment of type 2 diabetes mellitus (T2DM). A class of triazole GPR142 agonists was discovered through a high throughput screen. The lead compound
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05666abdc0e69d7961b4edf099a12f0b
https://europepmc.org/articles/PMC5150677/
https://europepmc.org/articles/PMC5150677/
Autor:
Janet Kerr, Gary G. Chicchi, Margaret Wu, Cai Li, Shuwen He, Vijay Bhasker G. Reddy, Sharon Tong, William K. Hagmann, Patrick Fitzgerald, Guillermo Fernandez, Andrew D. Howard, Tianying Jian, Zhe Feng, Raman K. Bakshi, Dorina Trusca, Peter H. Dobbelaar, Donald Nelson, Mikhail Reibarkh, Qing Shao, Liangqin Guo, Yun-Ping Zhou, Ravi P. Nargund, Kwei-Lan Tsao, Edward C. Sherer, Stan Mitelman, Pierre Morissette, Maria E. Trujillo, Quang Truong, Zhixiong Ye, James D. Dellureficio, Hongbo Qi, Melissa Lin, Shrenik K. Shah, Sylvia Volksdorf, Jian Liu, Qingmei Hong, Koppara Samuel, Alexander Pasternak, George J. Eiermann, Patricia B. Bunting, Wu Du, Bei B. Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(6)
MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs. Additional investigations revealed that the CV liability (QTc prolongation) was caused by the hERG off-target activity
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6412732d83fd31156d7974bed1994494
https://pubmed.ncbi.nlm.nih.gov/26898814
https://pubmed.ncbi.nlm.nih.gov/26898814
Autor:
Palucki Brenda, Patrick G. Pollard, Liangqin Guo, Tung M. Fong, Matthew J. Wyvratt, Randy R. Miller, Shuwen He, Constantin Tamvakopoulos, Iyassu K. Sebhat, Qianping Peng, Ravi P. Nargund, Zhixiong Ye, Airu S. Chen, Doreen E. Cashen, David H. Weinberg, Min K. Park, Raman K. Bakshi, D. Euan MacIntyre, Howard Y. Chen, Rui Tang, Tanya MacNeil, Qingmei Hong, Alison M. Strack, Ralph A. Stearns, Jian Liu, William J. Martin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2330-2334
We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound 1 shows anti-obesity efficacy without potentiating erectile activity in the rodent models.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99aea0aa624d82cc9bc8f3cfa4bdb369
https://doi.org/10.1016/j.bmcl.2011.02.090
https://doi.org/10.1016/j.bmcl.2011.02.090
Autor:
Yingjie Lai, Ralph A. Stearns, Qianping Peng, Ravi P. Nargund, Qingmei Hong, Jian Liu, Rui Tang, Matthew J. Wyvratt, Raman K. Bakshi, Randy R. Miller, Tianying Jian, Alison M. Strack, Tanya MacNeil, Liangqin Guo, Howard Y. Chen, James Dellureficio, Iyassu K. Sebhat, Peter H. Dobbelaar, Airu S. Chen, Constantin Tamvakopoulos, David H. Weinberg, Tung M. Fong, Christopher L. Franklin, Shuwen He, Zhixiong Ye
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4399-4405
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b04db1e6e6855a321002bb787613d21e
https://doi.org/10.1016/j.bmcl.2010.06.062
https://doi.org/10.1016/j.bmcl.2010.06.062
Autor:
Howard Y. Chen, William J. Martin, D. Euan MacIntyre, Zhixiong Ye, Raman K. Bakshi, Alison M. Strack, Doreen E. Cashen, Jian Liu, Yingjie Lai, Tianying Jian, Constantin Tamvakopoulos, Nancy N. Tsou, Shuwen He, James Dellureficio, Tung M. Fong, Peter H. Dobbelaar, David H. Weinberg, Airu S. Chen, Qingmei Hong, Iyassu K. Sebhat, Tanya MacNeil, Christopher L. Franklin, Ravi P. Nargund, Ralph A. Stearns, Rui Tang, Richard G. Ball, Matthew J. Wyvratt, Randy R. Miller, Liangqin Guo, Qianping Peng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:2106-2110
We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4 receptor agonist. Compound 1 shows excellent erectogenic activity in the rodent models.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5ecb491322cadefd63c62faedffb60b8
https://doi.org/10.1016/j.bmcl.2010.02.058
https://doi.org/10.1016/j.bmcl.2010.02.058
Autor:
Heather L. Sings, Mark T. Goulet, Matthew J. Wyvratt, Iyassu K. Sebhat, Liangqin Guo, Rui Tang, Ravi P. Nargund, Qianping Peng, Euan Macintyre, Feroze Ujjainwalla, Constantin Tamvakopoulos, Zhixiong Ye, Lex H.T. Van der Ploeg, David H. Weinberg, Tanya MacNeil, John Huber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3242-3247
Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is disclosed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df57b635925179aebc3ae868f442a4cc
https://doi.org/10.1016/j.bmcl.2008.04.049
https://doi.org/10.1016/j.bmcl.2008.04.049