Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Gregori J, Morriello"'
Autor:
David A. Candito, Vladimir Simov, Anmol Gulati, Solomon Kattar, Ryan W. Chau, Blair T. Lapointe, Joey L. Methot, Duane E. DeMong, Thomas H. Graham, Ravi Kurukulasuriya, Mitchell H. Keylor, Ling Tong, Gregori J. Morriello, John J. Acton, Barbara Pio, Weiguo Liu, Jack D. Scott, Michael J. Ardolino, Theodore A. Martinot, Matthew L. Maddess, Xin Yan, Hakan Gunaydin, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Hongshi Yu, Ellen C. Minnihan, Charles A. Lesburg, Ping Liu, Jing Su, Laxminarayan G. Hegde, Lily Y. Moy, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul Ciaccio, Jennifer A. Piesvaux, Karin M. Otte, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Santhosh Neelamkavil, Harold B. Wood, Peter H. Fuller, J. Michael Ellis
Publikováno v:
Journal of Medicinal Chemistry. 65:16801-16817
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::365ba0e1a6a6d085b4344b637344b726
https://doi.org/10.1021/acs.jmedchem.2c01605
https://doi.org/10.1021/acs.jmedchem.2c01605
Autor:
David A, Candito, Vladimir, Simov, Anmol, Gulati, Solomon, Kattar, Ryan W, Chau, Blair T, Lapointe, Joey L, Methot, Duane E, DeMong, Thomas H, Graham, Ravi, Kurukulasuriya, Mitchell H, Keylor, Ling, Tong, Gregori J, Morriello, John J, Acton, Barbara, Pio, Weiguo, Liu, Jack D, Scott, Michael J, Ardolino, Theodore A, Martinot, Matthew L, Maddess, Xin, Yan, Hakan, Gunaydin, Rachel L, Palte, Spencer E, McMinn, Lisa, Nogle, Hongshi, Yu, Ellen C, Minnihan, Charles A, Lesburg, Ping, Liu, Jing, Su, Laxminarayan G, Hegde, Lily Y, Moy, Janice D, Woodhouse, Robert, Faltus, Tina, Xiong, Paul, Ciaccio, Jennifer A, Piesvaux, Karin M, Otte, Matthew E, Kennedy, David Jonathan, Bennett, Erin F, DiMauro, Matthew J, Fell, Santhosh, Neelamkavil, Harold B, Wood, Peter H, Fuller, J Michael, Ellis
Publikováno v:
Journal of medicinal chemistry. 65(24)
Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically supported, chemically tractable, and potentially disease-modifying mechanism to treat Parkinson's disease. Herein, we describe the optimization of a novel ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::d1e71dbb505d333749f04ff7e2a07818
https://pubmed.ncbi.nlm.nih.gov/36475697
https://pubmed.ncbi.nlm.nih.gov/36475697
Autor:
Derun Li, William P. Kaplan, Cayetana Zarate, Matthew L. Maddess, Kaitlyn Marie Logan, Hongming Li, Peter Fuller, Zhiguo Jake Song, Meng Chen, Michael J. Ardolino, Jing Su, Luis E. Torres, Gregori J. Morriello
Publikováno v:
Organic Process Research & Development. 25:642-647
The application of bicyclo[1.1.1]pentanes (BCPs) as phenyl bioisosteres has garnered significant attention, as these structural motifs can improve the physiochemical profiles of drug candidates. De...
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b5496f6d6a0a0b3fe6cf13ba92f017ee
https://doi.org/10.1021/acs.oprd.0c00446
https://doi.org/10.1021/acs.oprd.0c00446
Autor:
Mitchell H. Keylor, Anmol Gulati, Solomon D. Kattar, Rebecca E. Johnson, Ryan W. Chau, Kaila A. Margrey, Michael J. Ardolino, Cayetana Zarate, Kelsey E. Poremba, Vladimir Simov, Gregori J. Morriello, John J. Acton, Barbara Pio, Xin Yan, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Charles A. Lesburg, Donovon Adpressa, Shishi Lin, Santhosh Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul J. Ciaccio, Jennifer Piesvaux, Karin M. Otte, Harold B. Wood, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Peter H. Fuller
Publikováno v:
Journal of medicinal chemistry. 65(1)
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder whose current therapies are limited in scope and efficacy. In this repor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6720c280fccf3e18653a864a196348ad
https://pubmed.ncbi.nlm.nih.gov/34967623
https://pubmed.ncbi.nlm.nih.gov/34967623
Autor:
Pravien Abeywickrema, Shawn J. Stachel, Tamara D. Cabalu, Anthony T. Ginetti, Yili Chen, Daniel V. Paone, Michael P. Dwyer, Jonathan E. Wilson, Deping Wang, Alejandro Crespo, Jun Lu, Christopher Joseph Sinz, Gregori J. Morriello, Shimin Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 44:128082
A focused SAR study was conducted on a series of N1-substituted pyrazolopyrimidinone PDE2 inhibitors to reveal compounds with excellent potency and selectivity. The series was derived from previously identified internal leads and designed to enhance
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33cfdd9f39e9f739df7e6d6ec5a403b0
https://doi.org/10.1016/j.bmcl.2021.128082
https://doi.org/10.1016/j.bmcl.2021.128082
Autor:
Carolyn Bahnck-Teets, Xu Min, Lehua Chang, Tracy L. Diamond, M. Katharine Holloway, John F. Fay, David Jonathan Bennett, John A. Mccauley, Jurgen Schulz, Marie Loughran, Peter D. Williams, Alejandro Crespo, Andrew Stamford, Hua-Poo Su, Michael D. Miller, Kartik M. Keertikar, Christopher J. Bungard, Catherine M. Wiscount, Bin Zhong, Jeanine E. Ballard, Sherman T. Waddell, Steven S. Carroll, Tao Ji, Jesse J. Manikowski, Bin Hu, Xin-jie Chu, Gregori J. Morriello, William J. Morris, Michael P. Dwyer
Publikováno v:
ACS Medicinal Chemistry Letters. 8:1292-1297
Using the HIV-1 protease binding mode of MK-8718 and PL-100 as inspiration, a novel aspartate binding bicyclic piperazine sulfonamide core was designed and synthesized. The resulting HIV-1 protease inhibitor containing this core showed an 60-fold inc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6240d0128d9c35a558caa2cfbba15fa5
https://doi.org/10.1021/acsmedchemlett.7b00386
https://doi.org/10.1021/acsmedchemlett.7b00386
Autor:
Richard G. Ball, Sheila M. Galloway, Katherine K. McGettigan, Harvey R. Wendt, Gregori J. Morriello, Jerry Di Salvo, Marat Vijay Reddy, Black Regina M, Amanda L. Hurley, Judy Morris, Scott D. Feighner, Eric Streckfuss, George A. Doss, Alka Bansal, Anthony Sanfiz, Scott D. Edmondson, Mary Struthers, Nancy N. Tsou, Jiafang He, Crystal McKnight, George M. Laws, Donna L. Hreniuk, Gino Salituro
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1865-1870
A novel class of human β(3)-adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β(3)-AR agonists. As observed, many of the β(3)-AR agonists seem to need the acyclic ethanolam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f6c8507b7efbb2f70d1c735a63653c9
https://doi.org/10.1016/j.bmcl.2010.12.087
https://doi.org/10.1016/j.bmcl.2010.12.087
Autor:
Richard Jiao, Pasquale P. Vicario, Gabor Butora, Shankaran Kothandaraman, Stephen D. Goble, Mary Struthers, Gregori J. Morriello, Julie A. DeMartino, Sander G. Mills, Malcolm MacCoss, Julia M. Ayala, Margaret A. Cascieri, Karla L. Donnely, Changyou Zhou, Lihu Yang, Alexander Pasternak
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1830-1834
A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37cf3150520d0f4c125edd804b8e5959
https://doi.org/10.1016/j.bmcl.2008.12.050
https://doi.org/10.1016/j.bmcl.2008.12.050
Autor:
Peter Lin, Gary G. Chicchi, Julie A. DeMartino, Neil Collinson, Marc M. Kurtz, Susan Boyce, Robert J. DeVita, Alan Wheeldon, Jonathan R. Young, Stephen Moore, Emma J. Carlson, Kwei-Lan C. Tsao, Sander G. Mills, Karen Townson, George A. Doss, Gregori J. Morriello, Nadia M.J. Rupniak
Publikováno v:
Bioorganic & Medicinal Chemistry. 16:2156-2170
Previous work on human NK(1) antagonists in which the core of the structure is a substituted pyrrolidine has been disclosed. These compounds showed good binding affinity and functional IP activity, however, many did not exhibit the necessary brain pe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a07bdec5af551942f4ff8d7149d7c129
https://doi.org/10.1016/j.bmc.2007.11.081
https://doi.org/10.1016/j.bmc.2007.11.081
Autor:
Beata Zamlynny, Stuart A. Green, Karen H. Dingley, Liping Wang, Ann E. Weber, Katherine L. Villa, Amanda L. Hurley, Dong-Ming Shen, Gregori J. Morriello, Scott D. Edmondson, Sookhee Ha, Anthony Sanfiz, Dorothy Levorse, Nam Fung Kar, Beatrice Sacre-Salem, Hiroshi Nagabukuro, Nina Jochnowitz, Aileen Fitzmaurice, Gino Salituro, Tara L. Frenkl, Jerry Di Salvo, Richard G. Ball, Loise Gichuru, James D. Ormes, Cheng Zhu, Christopher Moyes, Stephen D. Goble, Randy R. Miller, Mary Struthers, Bart Harper, Shruty Mistry, Andra S. Stevenson, Richard A. Berger
Publikováno v:
Journal of medicinal chemistry. 59(2)
The discovery of vibegron, a potent and selective human β3-AR agonist for the treatment of overactive bladder (OAB), is described. An early-generation clinical β3-AR agonist MK-0634 (3) exhibited efficacy in humans for the treatment of OAB, but dev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f522169161222843c23eb180bd9c7b46
https://pubmed.ncbi.nlm.nih.gov/26709102
https://pubmed.ncbi.nlm.nih.gov/26709102