Zobrazeno 1 - 10
of 25
pro vyhledávání: '"Peter G. Klimko"'
Autor:
Peter G. Klimko, Najam A. Sharif
Publikováno v:
British Journal of Pharmacology. 176:1051-1058
Topical ophthalmic formulations of analogues of the endogenous arachidonic acid cyclooxygenase metabolite, PGF(2α), are the standard of care treatment for the blinding disease glaucoma. These are the most potent and efficacious medical therapies for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38884c4d8b83ed9d387ce1317f6b1569
https://doi.org/10.1111/bph.14327
https://doi.org/10.1111/bph.14327
Publikováno v:
Drug Metabolism Letters. 11
Background 4-(piperazin-1-yl)-8-(trifluoromethyl)pyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazine (1) is a small-molecule which demonstrated a sub-nM inhibitory potency toward the histamine H4 receptor (H4R). However, it was found to be mutagenic in an in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec3e8bf5ceb9b446a458abff5a8109e8
https://doi.org/10.2174/1872312811666171106151730
https://doi.org/10.2174/1872312811666171106151730
Autor:
Peter G. Klimko, Najam A. Sharif
Publikováno v:
British journal of pharmacology. 176(8)
In contrast to the availability of potent and selective antagonists of several prostaglandin receptor types (including DP(1), DP(2), EP and TP receptors), there has been a paucity of well‐characterized, selective FP receptor antagonists. The earlie
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::14aa2364ee4b034d828aeab4e459609f
https://pubmed.ncbi.nlm.nih.gov/29679483
https://pubmed.ncbi.nlm.nih.gov/29679483
15(S)-Hydroxyeicosa-(5Z,8Z,11Z,13E)-tetraenoic acid (15(S)-HETE) is a metabolite of arachidonic acid that elicits a number of biological effects including vasoconstriction and angiogenesis. (5Z,11Z,15R)-15-Hydroxyeicosa-5,11-dien-13-ynoic acid (HETE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dcf1729ef6638bb7e8b6601a1ccaad62
https://europepmc.org/articles/PMC4893888/
https://europepmc.org/articles/PMC4893888/
Autor:
Peter G. Klimko, Najam A. Sharif
Publikováno v:
Expert Review of Ophthalmology. 4:477-489
The discovery of potent and efficacious intraocular pressure (IOP)-lowering FP-class prostaglandin (PG) analogs has revolutionized the treatment of ocular hypertension, a major risk factor for progression of the blinding disease glaucoma. Three isopr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::24d0677bfa44422efa89e15269d5ac7d
https://doi.org/10.1586/eop.09.40
https://doi.org/10.1586/eop.09.40
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
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
Publikováno v:
Journal of Medicinal Chemistry. 43:3400-3407
The racemic cyclohexane-for-cyclopentane ring substitution analogue of the potent prostaglandin FP agonist cloprostenol (7) was synthesized from cyclohexenediol 11 in 21 steps and 0.07% yield. In a prostaglandin FP receptor-linked second-messenger as
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eb26fc937e2d74729bf27378aed49a0
https://doi.org/10.1021/jm990587w
https://doi.org/10.1021/jm990587w
Autor:
Julia M. Heerding, Venkat Raman, Charles S. Swindell, Hemalatha Venkataraman, Leera T. Rahman, Peter G. Klimko, Madhavi C. Chander
Publikováno v:
The Journal of Organic Chemistry. 61:1101-1108
A ten-linear-step construction of C-aromatic taxane diene 14 from ethyl isopropyl ketone, acryloyl chloride, and commercially available 8 is reported. This sequence concludes with an intramolecular pinacol coupling carried out on 13. 14 is oxidized b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9190ad545ed82cbd313603dcf02ef01
https://doi.org/10.1021/jo951935e
https://doi.org/10.1021/jo951935e