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Synthesis of Pyrazole-Based Macrocycles Leads to a Highly Selective Inhibitor for MST3.
Amrhein JA, Berger LM, Balourdas DI, Joerger AC, Menge A, Krämer A, Frischkorn JM, Berger BT, Elson L, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T. Amrhein JA, et al. Among authors: kaiser a. J Med Chem. 2024 Jan 11;67(1):674-690. doi: 10.1021/acs.jmedchem.3c01980. Epub 2023 Dec 21. J Med Chem. 2024. PMID: 38126712
Aminothiazole-featured pirinixic acid derivatives as dual 5-lipoxygenase and microsomal prostaglandin E2 synthase-1 inhibitors with improved potency and efficiency in vivo.
Hanke T, Dehm F, Liening S, Popella SD, Maczewsky J, Pillong M, Kunze J, Weinigel C, Barz D, Kaiser A, Wurglics M, Lämmerhofer M, Schneider G, Sautebin L, Schubert-Zsilavecz M, Werz O. Hanke T, et al. Among authors: kaiser a. J Med Chem. 2013 Nov 27;56(22):9031-44. doi: 10.1021/jm401557w. Epub 2013 Nov 15. J Med Chem. 2013. PMID: 24171493
Anthranilic acid derivatives as novel ligands for farnesoid X receptor (FXR).
Merk D, Gabler M, Gomez RC, Flesch D, Hanke T, Kaiser A, Lamers C, Werz O, Schneider G, Schubert-Zsilavecz M. Merk D, et al. Among authors: kaiser a. Bioorg Med Chem. 2014 Apr 15;22(8):2447-60. doi: 10.1016/j.bmc.2014.02.053. Epub 2014 Mar 15. Bioorg Med Chem. 2014. PMID: 24685112
N-Benzylbenzamides: A Novel Merged Scaffold for Orally Available Dual Soluble Epoxide Hydrolase/Peroxisome Proliferator-Activated Receptor γ Modulators.
Blöcher R, Lamers C, Wittmann SK, Merk D, Hartmann M, Weizel L, Diehl O, Brüggerhoff A, Boß M, Kaiser A, Schader T, Göbel T, Grundmann M, Angioni C, Heering J, Geisslinger G, Wurglics M, Kostenis E, Brüne B, Steinhilber D, Schubert-Zsilavecz M, Kahnt AS, Proschak E. Blöcher R, et al. Among authors: kaiser a. J Med Chem. 2016 Jan 14;59(1):61-81. doi: 10.1021/acs.jmedchem.5b01239. Epub 2015 Dec 25. J Med Chem. 2016. PMID: 26595749
Characterization of the molecular mechanism of 5-lipoxygenase inhibition by 2-aminothiazoles.
Kretschmer SB, Woltersdorf S, Vogt D, Lillich FF, Rühl M, Karas M, Maucher IV, Roos J, Häfner AK, Kaiser A, Wurglics M, Schubert-Zsilavecz M, Angioni C, Geisslinger G, Stark H, Steinhilber D, Hofmann B. Kretschmer SB, et al. Among authors: kaiser a. Biochem Pharmacol. 2017 Jan 1;123:52-62. doi: 10.1016/j.bcp.2016.09.021. Epub 2016 Sep 23. Biochem Pharmacol. 2017. PMID: 27671344
Nonacidic Farnesoid X Receptor Modulators.
Flesch D, Cheung SY, Schmidt J, Gabler M, Heitel P, Kramer J, Kaiser A, Hartmann M, Lindner M, Lüddens-Dämgen K, Heering J, Lamers C, Lüddens H, Wurglics M, Proschak E, Schubert-Zsilavecz M, Merk D. Flesch D, et al. Among authors: kaiser a. J Med Chem. 2017 Aug 24;60(16):7199-7205. doi: 10.1021/acs.jmedchem.7b00903. Epub 2017 Aug 8. J Med Chem. 2017. PMID: 28749691
Allosteric modulation of the farnesoid X receptor by a small molecule.
Gabler M, Kramer J, Schmidt J, Pollinger J, Weber J, Kaiser A, Löhr F, Proschak E, Schubert-Zsilavecz M, Merk D. Gabler M, et al. Among authors: kaiser a. Sci Rep. 2018 May 1;8(1):6846. doi: 10.1038/s41598-018-25158-5. Sci Rep. 2018. PMID: 29717168 Free PMC article.
1,246 results