Zobrazeno 1 - 10
of 46
pro vyhledávání: '"A. R. Hellberg"'
Autor:
Abdelmoula Namil, Mark R. Hellberg, Andrew Rusinko, Bryon S. Severns, Jennifer Ward, Colene Drace, Iok-Hou Pang, Shenouda Yacoub, Keith D. Combrink, Curtis R. Kelly, Byron Li, Marsha A. McLaughlin, Raj Patil, N.A. Sharif, Hwang Hsing Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1875-1879
A series of 2,3,6-pyrazine Rho Kinase inhibitors were optimized for in vivo activity for topical ocular dosing. Modifications of the 2-(piperazin-1-yl)pyrazine derivatives produced compounds with improved solubility and physicochemical properties. Mo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d182bc1267668fdba6283e228caac75f
https://doi.org/10.1016/j.bmcl.2014.03.017
https://doi.org/10.1016/j.bmcl.2014.03.017
Autor:
Mark R. Hellberg, Colene Drace, Mark Hadden, Raj Patil, Marsha A. McLaughlin, Andrew Rusinko, Cheng Guo, Alan J. Henderson, N.A. Sharif, Decornez Helene, Neema Douglas
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1137-1140
Inhibition of rho kinase (ROCK) has been recognized as an important target for a number of diseases, including glaucoma. Herein we report SAR development around two hits from a kinase library that led to the discovery of the ROCK inhibitor compound 3
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fbb48a6520b9d4028267e693f42a6168
https://doi.org/10.1016/j.bmcl.2009.12.012
https://doi.org/10.1016/j.bmcl.2009.12.012
Autor:
Daniel Scott, Mark R. Hellberg, Tony Wallace, Najam A. Sharif, Gary W. Williams, Zixia Feng, Marsha A. McLaughlin
Publikováno v:
Bioorganic & Medicinal Chemistry. 17:576-584
FP-Class prostaglandin analogs have demonstrated utility for the treatment of glaucoma and ocular hypertension. A series of novel FP prostaglandin analogs was designed to optimize topical ocular activity and reduce ocular side-effects by replacing 13
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f37d1ab3784bbd5842cf333c733d5680
https://doi.org/10.1016/j.bmc.2008.11.070
https://doi.org/10.1016/j.bmc.2008.11.070
Autor:
Mark R. Hellberg, Bryon S. Severns, William F. Holt, Richard Young, Richard A. Glennon, Thomas R. Dean, Najam A. Sharif, Hwang-Hsing Chen, Curtis R. Kelly, Marsha A. McLaughlin, Jesse A. May
Publikováno v:
Journal of medicinal chemistry. 58(22)
Recently, it has been reported that 5-HT2 receptor agonists effectively reduce intraocular pressure (IOP) in a nonhuman primate model of glaucoma. Although 1-[(2S)-2-aminopropyl]indazol-6-ol (AL-34662) was shown to have good efficacy in this nonhuman
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4efded27acf90f8c38ea878165340de3
https://pubmed.ncbi.nlm.nih.gov/26551970
https://pubmed.ncbi.nlm.nih.gov/26551970
Autor:
Zixia Feng, Tom Brittain, Mark R. Hellberg, Grant Carr, Jesse A. May, Macarena Irigoyen, Damon Colbert, Shouxi Xu, Alfred N. Van Hoek, Peter M. Brown, Rajkumar V. Patil, Alok K. Mitra, Kulandaiappan Varadaraj, M. B. Wax, Andrew Rusinko, Najam A. Sharif, S. Sindhu Kumari
Publikováno v:
Chemical biologydrug design. 87(5)
Aquaporins (AQPs) are a family of membrane proteins that function as channels facilitating water transport in response to osmotic gradients. These play critical roles in several normal physiological and pathological states and are targets for drug di
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca01fb7cf84bf488e1c14a50826c5a8e
https://pubmed.ncbi.nlm.nih.gov/26685080
https://pubmed.ncbi.nlm.nih.gov/26685080
AL-12182, a novel 11-oxa prostaglandin analog with topical ocular hypotensive activity in the monkey
Autor:
Raymond E. Conrow, Mark R. Hellberg, David Earnest, Gary W. Williams, Pete Delgado, W. Dennis Dean, Najam A. Sharif, Peter G. Klimko, Michael S. Gaines, Karen S. Haggard, Robert D. Selliah, Marsha A. McLaughlin, Daniel Scott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:4525-4528
A series of 11-oxa prostaglandin analogs was evaluated for FP receptor binding and activation. Several compounds having aryloxy-terminated lower chains were found to be potent agonists. Topical ocular dosing of AL-12182, the isopropyl ester prodrug o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9eaa7f878c1b411bce26660af3350532
https://doi.org/10.1016/j.bmcl.2004.06.037
https://doi.org/10.1016/j.bmcl.2004.06.037
Autor:
Mark R. Hellberg, Karen S. Haggard, Gary W. Williams, John B. Liao, Peter G. Klimko, Marsha A. McLaughlin, Bryon S. Severns, Najam A. Sharif
Publikováno v:
Bioorganic & Medicinal Chemistry. 12:3451-3469
A novel series of 15-fluoro prostaglandins with phenoxy termination of the omega-chain was synthesized and evaluated for binding and functional activation of the prostaglandin FP receptor in vitro and for side effect potential and topical ocular hypo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd3f4077fe51bf4946881e500b817cc4
https://doi.org/10.1016/j.bmc.2004.04.034
https://doi.org/10.1016/j.bmc.2004.04.034
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 306:301-309
Published investigations of serotonin-1A (5-hydroxytryptamine1A; 5-HT1A) receptor agonists and serotonin-2A (5-hydroxytryptamine2A; 5-HT2A) receptor antagonists in nonprimate species provide conflicting results with regard to their intraocular pressu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::566796ff9d0a2440ed74560989adbd03
https://doi.org/10.1124/jpet.103.049528
https://doi.org/10.1124/jpet.103.049528
Autor:
Thomas R. Dean, Gustav Graff, Mark R. Hellberg, Tai-Lee Ke, Peter G. Klimko, Karen S. Haggard
Publikováno v:
Journal of Ocular Pharmacology and Therapeutics. 19:97-103
Bimatoprost (Lumigan), the ethyl amide derivative of the potent prostaglandin FP agonist 17-phenyl-trinor PGF(2alpha), has been reported to be a member of a pharmacologically unique class of ocular hypotensive agents. To confirm that bimatoprost, whi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58a7e914b5976b441ce74f6459db603a
https://doi.org/10.1089/108076803321637627
https://doi.org/10.1089/108076803321637627
Autor:
Lori K. Weimer, Mark R. Hellberg, Karen C. David, Jon C. Nixon, Gustav Graff, Milton T. Brady
Publikováno v:
Inflammation. 27:31-43
Selected ester- (AL-5898 and AL-8417) and amide-linked benzopyran analogues (AL-7538 and AL-12615) were evaluated in vitro for their ability to inhibit key enzymes/processes of the inflammatory response. AL-7538 and AL-12615 exhibited weak intrinsic
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::179ae35c7c57807e982558efc70518f7
https://doi.org/10.1023/a:1022687111884
https://doi.org/10.1023/a:1022687111884