Zobrazeno 1 - 10
of 46
pro vyhledávání: '"Xiaoliang, Zhuo"'
Autor:
Ying Wang, Jack Krupinski, Gary G. Cao, Xiaoliang Zhuo, Joseph Carpenter, Erica Cook, Milinda Ziegler, Karen A. Rossi, Anthony V. Azzara, Kathy Mosure, Gang Wu, Matthew G. Soars, Dean A. Wacker, Bruce A. Ellsworth, Doree F. Sitkoff, Tao Wang
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein we report the discovery and preclinical biological evaluation of 6-(2-(5-cyclopropyl-3-(3,5-dichloropyridin-4-yl)isoxazol-4-yl)-7-azaspiro[3.5]non-1-en-7-yl)-4-(trifluoromethyl)quinoline-2-carboxylic acid, compound 1 (BMS-986
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce42c1d64be61d8389ebf3b9000ba19f
https://doi.org/10.1021/acsmedchemlett.1c00198
https://doi.org/10.1021/acsmedchemlett.1c00198
Autor:
Susheel J. Nara, Srinivas Jogi, Srinivas Cheruku, Sarkunam Kandhasamy, Firoz Jaipuri, Pavan Kalyan Kathi, Subba Reddy, Sanket Sarodaya, Erica M. Cook, Tao Wang, Doree Sitkoff, Karen A. Rossi, Max Ruzanov, Susan E. Kiefer, Javed A. Khan, Mian Gao, Satyanarayana Reddy, Sankara Sivaprasad LVJ, Ramola Sane, Kathy Mosure, Xiaoliang Zhuo, Gary G. Cao, Milinda Ziegler, Anthony Azzara, John Krupinski, Matthew G. Soars, Bruce A. Ellsworth, Dean A. Wacker
Publikováno v:
Journal of medicinal chemistry. 65(13)
While several farnesoid X receptor (FXR) agonists under clinical investigation for the treatment of nonalcoholic steatohepatitis (NASH) have shown beneficial effects, adverse effects such as pruritus and elevation of plasma lipids have limited their
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::950a84b56e656ee81f551db19a874f2a
https://pubmed.ncbi.nlm.nih.gov/35704802
https://pubmed.ncbi.nlm.nih.gov/35704802
Publikováno v:
Journal of Medicinal Chemistry. 63:6315-6386
The applications of fluorine in drug design continue to expand, facilitated by an improved understanding of its effects on physicochemical properties and the development of synthetic methodologies that are providing access to new fluorinated motifs.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e98b140acbca433aab2e1d86dcadc076
https://doi.org/10.1021/acs.jmedchem.9b01877
https://doi.org/10.1021/acs.jmedchem.9b01877
Autor:
John E. Macor, Yunhui Zhang, James E. Grace, Lorin A. Thompson, Jeremy H. Toyn, Lawrence R. Marcin, Subramaniam Krishnananthan, Jianliang Shi, Dmitry Zuev, Daniel Smith, Jianqing Li, Yong-Jin Wu, Jason M. Guernon, Xiaoliang Zhuo, Tatyana Zvyaga, Xu Li, Arvind Mathur, John Morrison, Jere E. Meredith, Charles F. Albright, S. Roy Kimura, Mendi A. Higgins, Kimberley A. Lentz, Richard E. Olson, Rex Denton, Kenneth M. Boy, Catherine R. Burton, Ashok K. Trehan, Michael K. Ahlijanian
Publikováno v:
ACS Medicinal Chemistry Letters
A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the bicyclic pyrimidine γ-secretase modulator BMS-932481. The compound showed robust reductions of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed62d494eee5e78e1c6f0f7838951135
http://europepmc.org/articles/PMC6421538
http://europepmc.org/articles/PMC6421538
Autor:
Jeremy H. Toyn, Lorin A. Thompson, Kimberley A. Lentz, Jere E. Meredith, Catherine R. Burton, Sethu Sankaranararyanan, Valerie Guss, Tracey Hall, Lawrence G. Iben, Carol M. Krause, Rudy Krause, Xu-Alan Lin, Maria Pierdomenico, Craig Polson, Alan S. Robertson, R. Rex Denton, James E. Grace, John Morrison, Joseph Raybon, Xiaoliang Zhuo, Kimberly Snow, Ramesh Padmanabha, Michele Agler, Kim Esposito, David Harden, Margaret Prack, Sam Varma, Victoria Wong, Yingjie Zhu, Tatyana Zvyaga, Samuel Gerritz, Lawrence R. Marcin, Mendi A. Higgins, Jianliang Shi, Cong Wei, Joseph L. Cantone, Dieter M. Drexler, John E. Macor, Richard E. Olson, Michael K. Ahlijanian, Charles F. Albright
Publikováno v:
International Journal of Alzheimer's Disease, Vol 2014 (2014)
Alzheimer’s disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid Aβ1-42, in the brain. Aβ1-42 levels can be decreased by γ-secretase modulators (GSM), whi
Externí odkaz:
https://doaj.org/article/1dce320132d4411583a19dcbfe2b54ae
Autor:
Xiaoliang Zhuo1, Ying-Zi Wang1, Xiaohua Stella Huang1, Yue-Zhong Shu1, Johnson, Benjamin M.1, Kap-Sun Yeung2, Juliang Zhu2, Parcella, Kyle E.2, Eastman, Kyle J.2, Kadow, John F.2, Meanwell, Nicholas A.2
Publikováno v:
Xenobiotica. Dec2018, Vol. 48 Issue 12, p1215-1226. 12p.
Autor:
Xiaohua Stella Huang, Kyle J. Eastman, Kyle Parcella, Benjamin M. Johnson, John F. Kadow, Xiaoliang Zhuo, Juliang Zhu, Yue-Zhong Shu, Nicholas A. Meanwell, Kap-Sun Yeung, Yingzi Wang
Publikováno v:
Xenobiotica. 48:1215-1226
1. Due to its unique C-C and C-H bonding properties, conformational preferences and relative hydrophilicity, the cyclopropyl ring has been used as a synthetic building block in drug discovery to modulate potency and drug-like properties. During an ef
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::794e99f15e512d318d95a2229238dea7
https://doi.org/10.1080/00498254.2017.1409915
https://doi.org/10.1080/00498254.2017.1409915
Autor:
Dawn D. Parker, Karen Rigat, Kyle J. Eastman, Umesh Hanumegowda, Katharine A. Grant-Young, Nicholas A. Meanwell, Maria Tuttle, Tao Wang, Tatyana Zvyaga, Susan B. Roberts, Hua Fang, Kap-Sun Yeung, Mengping Liu, Julie A. Lemm, Kathy Mosure, Xiaoliang Zhuo, Maria Donoso, Kyle Parcella, Zhongxing Zhang, Matthew G. Soars, Zuzana Haarhoff, Zhiwei Yin, Ying-Kai Wang, John F. Kadow, Juliang Zhu
Publikováno v:
ACS Medicinal Chemistry Letters. 8:771-774
Iterative structure–activity analyses in a class of highly functionalized furo[2,3-b]pyridines led to the identification of the second generation pan-genotypic hepatitis C virus NS5B polymerase primer grip inhibitor BMT-052 (14), a potential clinic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::21db76c03898e00a9f3ff613bf9bd713
https://doi.org/10.1021/acsmedchemlett.7b00211
https://doi.org/10.1021/acsmedchemlett.7b00211
Autor:
Katherine A. Grant-Young, Andrew Nickel, Rajesh Onkardas Bora, Prakash Anjanappa, Bender John A, Kevin Kish, Kap-Sun Yeung, Dawn D. Parker, Joseph Raybon, Mark R. Witmer, Karen Rigat, Matthew G. Soars, Steven Sheriff, Yue-Zhong Shu, Kenneth S. Santone, Prashantha Gunaga, Kyle Parcella, Nicholas A. Meanwell, Jay O. Knipe, Susan B. Roberts, Alicia Ng, Michael Sinz, Kathy Mosure, Ying-Kai Wang, Brett R. Beno, Mengping Liu, Elizabeth Colston, Dennis M. Grasela, John F. Kadow, Qi Gao, Min Gao, Umesh Hanumegowda, Roy Haskell, Julie A. Lemm, Xiaoliang Zhuo, Changhong Wan, Kumaravel Selvakumar
Publikováno v:
Journal of Medicinal Chemistry. 60:4369-4385
The hepatitis C virus (HCV) NS5B replicase is a prime target for the development of direct-acting antiviral drugs for the treatment of chronic HCV infection. Inspired by the overlay of bound structures of three structurally distinct NS5B palm site al
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43e500f8c2cd73d6873f1280c193d753
https://doi.org/10.1021/acs.jmedchem.7b00328
https://doi.org/10.1021/acs.jmedchem.7b00328
Autor:
Andrew P. Degnan, Valerie J. Whiterock, Darrell Maxwell, Umesh Hanumegowda, Digavalli V. Sivarao, Anand Balakrishnan, Eric Shields, Joanne J. Bronson, Jeffrey M. Brown, Ryan Westphal, Amy Easton, Arun K. Senapati, Xiaoliang Zhuo, John E. Macor, Kenneth S. Santone, Michael Gulianello, Regina Miller, Melissa Hill-Drzewi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5871-5876
Schizophrenia is a serious illness that affects millions of patients and has been associated with N-methyl-d-aspartate receptor (NMDAR) hypofunction. It has been demonstrated that activation of metabotropic glutamate receptor 5 (mGluR5) enhances NMDA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6efc9c8447ba3a2d03837196eeccc095
https://doi.org/10.1016/j.bmcl.2016.11.014
https://doi.org/10.1016/j.bmcl.2016.11.014