Zobrazeno 1 - 10
of 52
pro vyhledávání: '"Chaozhong Cai"'
Design, synthesis and SAR of a novel series of heterocyclic phenylpropanoic acids as GPR120 agonists
Autor:
Austin Bell, Hong Hua, Wen Yan, Chaozhong Cai, Celia Jenkinson, Peter Haug, Wall Mark, Yuanping Wang, Imad Nashashibi, Xuqing Zhang, Arthur T. Suckow, Michael P. Winters, James N. Leonard, Michele Wells, Joseph Gunnet, William V. Murray, Zhihua Sui, Jingyuan Ma, James C. Lanter, Wilma Clapper, Aaron Novack
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:3272-3278
A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8c99a9954f694ac0a6035dcb18ac83bf
https://doi.org/10.1016/j.bmcl.2017.06.028
https://doi.org/10.1016/j.bmcl.2017.06.028
Autor:
Zhihua Sui, Yuanping Wang, Xuqing Zhang, Mark J. Macielag, Hong Hua, Wen Yan, Peter Haug, Austin Bell, Joseph Gunnet, Chaozhong Cai, Celia Jenkinson, William V. Murray, James N. Leonard, Arthur T. Suckow, Wilma Clapper
We have discovered a novel series of isothiazole-based phenylpropanoic acids as GPR120 agonists. Extensive structure–activity relationship studies led to the discovery of a potent GPR120 agonist 4x, which displayed good EC50 values in both calcium
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7ef3b314c5a726bc0646f755898f00a
https://europepmc.org/articles/PMC5601374/
https://europepmc.org/articles/PMC5601374/
Autor:
Shawn Branum, Fawzy Nagy E, Christopher A. Teleha, Luc Van Der Steen, Mark J. Wall, Derek A. Beauchamp, Michael Reuman, Marc Verbeek, Michael Kolpak, Zhihua Sui, Chaozhong Cai, Gregory C. Leo, Ronald K. Russell, Yongzheng Zhang, Fu-An Kang, Hilde Vanbaelen
Publikováno v:
Organic Process Research & Development. 18:1622-1629
The preparation of a novel chemokine receptor type 2 (CCR-2) antagonist is described on a 135 g scale. The synthesis of an all-carbon bicyclic core was accomplished using a radical cyclization strategy using chiral precursors, wherein elaboration led
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::30ed40727f516d73f0e1e4e53e8301d9
https://doi.org/10.1021/op500265z
https://doi.org/10.1021/op500265z
Autor:
Zhihua Sui, Cuifen Hou, Dave F. McComsey, Evan Opas, Dana L. Johnson, Sandra McKenney, John C. O’Neill, Chaozhong Cai
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1239-1242
SAR study of 5-aminooctahydrocyclopentapyrrole-3a-carboxamide scaffold led to identification of several CCR2 antagonists with potent activity in both binding and functional assays. Their cardiovascular safety and pharmacokinetic properties were also
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95515505e7d5f37a20cbc3f3ccd0edf4
https://doi.org/10.1016/j.bmcl.2013.05.024
https://doi.org/10.1016/j.bmcl.2013.05.024
Autor:
Zhihua Sui, Derek A. Beauchamp, Christopher A. Teleha, Ronald K. Russell, Chaozhong Cai, Fu-An Kang
Publikováno v:
Tetrahedron: Asymmetry. 24:651-656
Two cycloaddition methods were applied to chiral protected aminocyclopentenes 2 and 9 and provided novel bicyclic products 3 and 4 in good yields. The explanation for the observed stereochemistry was based on the sterically encumbered β-face forcing
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a63aa46f9ea716d2c141f8aca41fa9c1
https://doi.org/10.1016/j.tetasy.2013.04.014
https://doi.org/10.1016/j.tetasy.2013.04.014
Autor:
Chaozhong Cai, Alexey B. Dyatkin, Paul R. Wade, Kavash Robert W, Sui-Po Zhang, Henry J. Breslin, Craig J. Diamond, Wei He, Tamara A. Miskowski, Pamela J. Hornby
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4869-4872
A small set of acyclic analogs 5 were prepared to explore their structure-activity relationships (SARs) relative to heterocyclic core, opioid receptor (OR) agonists 4. Compound 5l was found to have very favorable OR binding affinities at the δ and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2c81ce41ee0795527efdfdb550ea3b0
https://doi.org/10.1016/j.bmcl.2012.05.042
https://doi.org/10.1016/j.bmcl.2012.05.042
Autor:
Zhihua Sui, Evan Opas, Cuifen Hou, Carl Crysler, Monica Singer, Xuqing Zhang, Dana L. Johnson, Chaozhong Cai, Hufnagel Heather Rae, Thomas P. Markotan, Sandra McKenney, James C. Lanter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:5577-5582
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13350ab536cad7aa9c759b2b60a1aa24
https://doi.org/10.1016/j.bmcl.2011.06.080
https://doi.org/10.1016/j.bmcl.2011.06.080
Autor:
Ling Lin, Chaozhong Cai, Christopher M. Flores, Timothy P Coogan, Edmund K. LeGrand, Ellen E. Codd, Raymond W. Colburn, Angelique Leone, Charles Y. Wang, Mcdonnell Mark E, Scott L. Dax, Michael R. Brandt, Stewart Bryant, Bart DeCorte, James J. McNally, John R. Mabus, Sui-Po Zhang, John R. Carson, Michael Kemmerer, Dennis J. Stone, James M Lenhard, Michael K. McMillian, Kristen M. Chevalier, Judith Baker
Publikováno v:
Toxicological Sciences. 117:493-504
The unexpected observation of a hyperglycemic effect of some tricycle-based delta opioid receptor (DOR) agonists led to a series of studies to better understand the finding. Single administration of two novel tricyclic DOR agonists dose dependently e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9776c107aa28aa0bdc15b9be77554703
https://doi.org/10.1093/toxsci/kfq200
https://doi.org/10.1093/toxsci/kfq200
Publikováno v:
Tetrahedron Letters. 45:6855-6858
Methyl N-(E-enoyl)pyroglutamates, derived from inexpensive and readily available in both enantiomeric forms pyroglutamic acid were found to be an efficient Michael acceptors in the addition reactions with nucleophilic glycine equivalent allowing for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::95b1fc5fe1b4805c54dd98b7ff9b41c2
https://doi.org/10.1016/j.tetlet.2004.07.096
https://doi.org/10.1016/j.tetlet.2004.07.096
Autor:
Christopher M. Cabello, Minying Cai, Alexander V. Mayorov, Chaozhong Cai, Jennifer R. Swift, D. Trivedi, Victor J. Hruby, Chiyi Xiong, V. A. Soloshonok
Publikováno v:
The Journal of Peptide Research. 63:116-131
To investigate the molecular basis for the interaction of the chi-constrained conformation of melanotropin peptide with the human melanocortin receptors, a series of beta-substituted proline analogs were synthesized and incorporated into the Ac-Nle-C
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::df88006487d2559696759be67d7c5375
https://doi.org/10.1111/j.1399-3011.2003.00105.x
https://doi.org/10.1111/j.1399-3011.2003.00105.x