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Page 1
[The history of ulcer treatment].
Syha Y, Popescu L, Wurglics M, Schubert-Zsilavecz M. Syha Y, et al. Pharm Unserer Zeit. 2005;34(3):188-92. doi: 10.1002/pauz.200500117. Pharm Unserer Zeit. 2005. PMID: 15940950 Review. German. No abstract available.
Structure optimization of a new class of PPARγ antagonists.
Hernandez-Olmos V, Knape T, Heering J, von Knethen A, Kilu W, Kaiser A, Wurglics M, Helmstädter M, Merk D, Schubert-Zsilavecz M, Parnham MJ, Steinhilber D, Proschak E. Hernandez-Olmos V, et al. Bioorg Med Chem. 2019 Nov 1;27(21):115082. doi: 10.1016/j.bmc.2019.115082. Epub 2019 Aug 27. Bioorg Med Chem. 2019. PMID: 31548084
It exhibits competitive antagonism against rosiglitazone mediated activation of PPARgamma ligand binding domain (PPARgammaLBD) in a transactivation assay in HEK293T cells with an IC(50) of 4.3 M against 1 M rosiglitazone. The aim of this study was to investigate the …
It exhibits competitive antagonism against rosiglitazone mediated activation of PPARgamma ligand binding domain (PPARgammaLBD) in a transact …
Structure-activity relationship and in vitro pharmacological evaluation of imidazo[1,2-a]pyridine-based inhibitors of 5-LO.
Buscató El, Wisniewska JM, Rödl CB, Brüggerhoff A, Kaiser A, Rörsch F, Kostewicz E, Wurglics M, Schubert-Zsilavecz M, Grösch S, Steinhilber D, Hofmann B, Proschak E. Buscató El, et al. Future Med Chem. 2013 May;5(8):865-80. doi: 10.4155/fmc.13.72. Future Med Chem. 2013. PMID: 23682565
Chemical modifications for lead optimization via straight forward synthesis was used to combine small polar groups, which led to a suitable candidate (IC50 [polymorphonuclear leukocytes] = 1.15 M, IC50 [S100] = 0.29 M) with desired in vitro biopharmaceutical profile …
Chemical modifications for lead optimization via straight forward synthesis was used to combine small polar groups, which led to a suitable …
Molecular pharmacological profile of a novel thiazolinone-based direct and selective 5-lipoxygenase inhibitor.
Hofmann B, Rödl CB, Kahnt AS, Maier TJ, Michel AA, Hoffmann M, Rau O, Awwad K, Pellowska M, Wurglics M, Wacker M, Zivković A, Fleming I, Schubert-Zsilavecz M, Stark H, Schneider G, Steinhilber D. Hofmann B, et al. Br J Pharmacol. 2012 Apr;165(7):2304-13. doi: 10.1111/j.1476-5381.2011.01707.x. Br J Pharmacol. 2012. PMID: 21955369 Free PMC article.
KEY RESULTS: C06 induced non-cytotoxic, direct 5-LOX inhibition with IC(50) values about 0.66 M (intact PMNL, PMNL homogenates) and approximately 0.3 M (cell-free PMNL S100, partially purified 5-LOX). ...
KEY RESULTS: C06 induced non-cytotoxic, direct 5-LOX inhibition with IC(50) values about 0.66 M (intact PMNL, PMNL homogenates) and a …
A pirinixic acid derivative (LP105) inhibits murine 5-lipoxygenase activity and attenuates vascular remodelling in a murine model of aortic aneurysm.
Revermann M, Mieth A, Popescu L, Paulke A, Wurglics M, Pellowska M, Fischer AS, Steri R, Maier TJ, Schermuly RT, Geisslinger G, Schubert-Zsilavecz M, Brandes RP, Steinhilber D. Revermann M, et al. Br J Pharmacol. 2011 Aug;163(8):1721-32. doi: 10.1111/j.1476-5381.2011.01321.x. Br J Pharmacol. 2011. PMID: 21410457 Free PMC article.
KEY RESULTS In a monocyte cell line (RAW264.7), LP105 inhibited 5-LOX in whole cells (IC(50) : 1-3 M) and in supernatants (IC(50) : 10 M). Oral administration of LP105 to mice resulted in therapeutic tissue and plasma levels. ...
KEY RESULTS In a monocyte cell line (RAW264.7), LP105 inhibited 5-LOX in whole cells (IC(50) : 1-3 M) and in supernatants (IC(50) : 1 …
Brain permeability of bilobalide as probed by microdialysis before and after middle cerebral artery occlusion in mice.
Lang D, Ude C, Wurglics M, Schubert-Zsilavecz M, Klein J. Lang D, et al. J Pharm Pharm Sci. 2010;13(4):607-14. doi: 10.18433/j31c7q. J Pharm Pharm Sci. 2010. PMID: 21486534 Free article.
Bilobalide was already detectable in brain striatal microdialysates 10 min after i.p. administration and reached maximum levels (19 ng/mL, corresponding to 0.92 M) after 40 min. Maximum plasma bilobalide levels were 5.9 M. After an ischemic insult, the drug could be …
Bilobalide was already detectable in brain striatal microdialysates 10 min after i.p. administration and reached maximum levels (19 ng/mL, c …
Development of a high-performance liquid chromatographic method with electrochemical detection for the determination of hyperforin.
Rückert U, Eggenreich K, Wintersteiger R, Wurglics M, Likussar W, Michelitsch A. Rückert U, et al. J Chromatogr A. 2004 Jul 2;1041(1-2):181-5. doi: 10.1016/j.chroma.2004.04.062. J Chromatogr A. 2004. PMID: 15281267
The hyperforin solutions were separated isocratically using a mobile phase consisting of 10% ammonium acetate buffer (0.5 M, pH 3.7)-MeOH-acetonitrile (10:40:50, v/v) at a flow rate of 0.8 mL/min. Hyperforin was detected amperometrically with a glassy carbon electrode at a …
The hyperforin solutions were separated isocratically using a mobile phase consisting of 10% ammonium acetate buffer (0.5 M, pH 3.7)- …