Zobrazeno 1 - 10
of 17
pro vyhledávání: '"Shawn P. Walsh"'
Autor:
Shawn P. Walsh, Lee-Yuh Pai, Yuping Zhu, John P. Felix, Caryn Hampton, Xiaoyan Zhou, Melba Hernandez, Brande Thomas-Fowlkes, Richard M. Brochu, Nardos Teumelsan, Gregory J. Kaczorowski, Emma R. Parmee, Maria L. Garcia, Alexander Pasternak, Jinlong Jiang, Sookhee Ha, Sophie Roy, Kathleen A. Sullivan, Haifeng Tang, Lihu Yang, Karen Owens, Reynalda K. de Jesus, Xin Gu, Birgit T. Priest, Barbara Pio, Fa-Xiang Ding, Andrew M. Swensen, Magdalena Alonso-Galicia, Aurash Shahripour, Juliann Ehrhart, Timothy Bailey
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:5695-5702
Following the discovery of small molecule acyl piperazine ROMK inhibitors, the acyl octahydropyrazino[2,1-c][1,4]oxazine series was identified. This series displays improved ROMK/hERG selectivity, and as a consequence, the resulting ROMK inhibitors d
Autor:
Hong Liu, Shawn P. Walsh, Yan Qi, Jiaqiang Cai, Jack D. Scott, Xin-Jie Chu, Cuizhi Mu, Brandon M. Taoka, Yaxian Cai, Jinsong Hao, Quang Truong, Zhong Lai, Xing Dai, Wen-Lian Wu, Jeffrey T. Kuethe, Eric J. Gilbert, Andrew Brunskill, Jared N. Cumming
Publikováno v:
Tetrahedron. 72:6011-6020
A novel domino reaction for the preparation of non-racemic β-proline derivatives is reported. The addition of a methyl 2-(oxetan-3-yl)acetate titanium enolate to chiral tert-butanesulfinyl ketimines followed by an intramolecular oxetane ring-opening
Autor:
Michael J. Forrest, John P. Felix, Lee-Yuh Pai, Melba Hernandez, Yuping Zhu, Aaron Corona, Joseph M. Metzger, Gregory J. Kaczorowski, Nardos Teumelsan, Lihu Yang, Karen Owens, Timothy Bailey, Caryn Hampton, Vincent Tong, Alexander Pasternak, Brande Thomas-Fowlkes, Shawn P. Walsh, Emma R. Parmee, Haifeng Tang, Richard M. Brochu, Maria L. Garcia, Xiaoyan Zhou, Magdalena Alonso-Galicia, Sophie Roy, Birgit T. Priest, Andrew M. Swensen, Aurash Shahripour
Publikováno v:
ACS Medicinal Chemistry Letters. 7:697-701
ROMK, the renal outer medullary potassium channel, is involved in potassium recycling at the thick ascending loop of Henle and potassium secretion at the cortical collecting duct in the kidney nephron. Because of this dual site of action, selective i
Autor:
Lee-Yuh Pai, Yuping Zhu, Richard Visconti, Xiaoyan Zhou, John P. Felix, Melba Hernandez, Jing Chen, Michael Margulis, Nardos Teumelsan, Sophie Roy, Kathleen A. Sullivan, Jessica Liu, Joseph M. Metzger, Aaron Corona, Gregory J. Kaczorowski, Maria L. Garcia, Lihu Yang, Shawn P. Walsh, Birgit T. Priest, Alexander Pasternak, Caryn Hampton, Emma R. Parmee, Vincent Tong, Brande Thomas-Fowlkes, Haifeng Tang, Magdalena Alonso-Galicia, Kashmira Shah, Michael J. Forrest, Richard M. Brochu, Ross Bentley, Sookhee Ha, Karen Owens, Aurash Shahripour, Andrew M. Swensen, Jessica Frie, Adam B. Weinglass, Timothy Bailey
Publikováno v:
ACS Medicinal Chemistry Letters. 6:747-752
A new subseries of ROMK inhibitors exemplified by 28 has been developed from the initial screening hit 1. The excellent selectivity for ROMK inhibition over related ion channels and pharmacokinetic properties across preclinical species support furthe
Autor:
Pamela K Carmines, Xiaoyan Zhou, Maya Dajee, Kathleen A Sullivan, Shawn P Walsh, Alexander Pasternak
Publikováno v:
Hypertension. 70
The bee venom toxin tertiapin Q (TPQ) evokes tubuloglomerular feedback-independent afferent arteriolar constriction in kidneys from rats with streptozotocin-induced type 1 diabetes (STZ rats). Because TPQ inhibits both Kir1.1 and Kir3.x channels, the
Autor:
Xiaoyan Zhou, Shawn P. Walsh, William J. Welch, Kathleen A. Sullivan, Magali Araujo, Alexander Pasternak, Christopher S. Wilcox
Publikováno v:
American journal of physiology. Renal physiology. 312(6)
The Na+-K+-2Cl−cotransporter (NKCC2) on the loop of Henle is the site of action of furosemide. Because outer medullary potassium channel (ROMK) inhibitors prevent reabsorption by NKCC2, we tested the hypothesis that ROMK inhibition with a novel sel
Autor:
Yan Yan, Richard M. Brochu, Maria L. Garcia, Lihu Yang, Sophie Roy, Gregory J. Kaczorowski, Reynald K. de Jesus, Birgit T. Priest, Xiaoyan Zhou, Lee-Yuh Pai, Shawn P. Walsh, Yuping Zhu, Karen Owens, Caryn Hampton, Timothy Bailey, Andrew M. Swensen, Brande Thomas-Fowlkes, Magdalena Alonso-Galicia, John P. Felix, Melba Hernandez, Alexander Pasternak, Haifeng Tang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:5829-5832
A sub-class of distinct small molecule ROMK inhibitors were developed from the original lead 1. Medicinal chemistry endeavors led to novel ROMK inhibitors with good ROMK functional potency and improved hERG selectivity. Two of the described ROMK inhi
Autor:
Xiaoyan Zhou, Maya Dajee, Michael J. Forrest, Gail Forrest, Sloan Stribling, Andra S. Stevenson, Shawn P. Walsh, Kathleen A. Sullivan, Yonghua Zhu, Wanda Sharif-Rodriguez, Daphne Szeto, Alexander Pasternak, Yuchen Zhou, Olga Urosevic-Price
Publikováno v:
Hypertension (Dallas, Tex. : 1979). 69(2)
The renal outer medullary potassium (ROMK) channel mediates potassium recycling and facilitates sodium reabsorption through the Na + /K + /2Cl − cotransporter in the loop of Henle and potassium secretion at the cortical collecting duct. Evidence fr
Autor:
Shawn P. Walsh, Jessica Frie, Nardos Teumelsan, Maria L. Garcia, Karen Owens, Sophie Roy, Caryn Hampton, Reynalda K. de Jesus, Birgit T. Priest, Magdalena Alonso-Galicia, Aurash Shahripour, Richard M. Brochu, Juliann Ehrhart, Andrew M. Swensen, Haifeng Tang, Timothy Bailey, Alexander Pasternak, Lee-Yuh Pai, Yuping Zhu, Lihu Yang, Gregory J. Kaczorowski, John P. Felix, Melba Hernandez, Brande Thomas-Fowlkes, Xiaoyan Zhou
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(9)
Following the discovery of small molecule acyl piperazine ROMK inhibitors and their initial preclinical validation as a novel diuretic agent, our group set out to discover new ROMK inhibitors with reduced risk for QT effects, suitable for further pha
Autor:
Min Shu, William J. Greenlee, Alan Hruza, Harold B. Wood, Min Park, Shawn P. Walsh, Kenneth P. Ellsworth, Yi-Heng Chen, Lisa M. Sonatore, Bart Harper, Bing Li, Aurash Sharipour, Richard A. Berger, Cameron J. Smith, Esther Kim, Edward C. Sherer, Paul Reichert, Jane Y. Wu, Wayne M. Geissler, Jiayi Xu, Sunita V. Dewnani, James M. Balkovec, Dann L. Parker, Ting Zhang
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(11)
Two high-throughput screening hits were investigated for SAR against human factor IXa. Both hits feature a benzamide linked to a [6-5]-heteroaryl via an alkyl amine. In the case where this system is a benzimidazolyl-ethyl amine the binding potency fo