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HTS-based discovery and optimization of novel positive allosteric modulators of the α7 nicotinic acetylcholine receptor.
Ledneczki I, Horváth A, Tapolcsányi P, Éles J, Molnár KD, Vágó I, Visegrády A, Kiss L, Szigetvári Á, Kóti J, Krámos B, Mahó S, Holm P, Kolok S, Fodor L, Thán M, Kostyalik D, Balázs O, Vastag M, Greiner I, Lévay G, Lendvai B, Némethy Z. Ledneczki I, et al. Among authors: kiss l. Eur J Med Chem. 2021 Oct 15;222:113560. doi: 10.1016/j.ejmech.2021.113560. Epub 2021 May 29. Eur J Med Chem. 2021. PMID: 34111828
Discovery of MK-1832, a Kv1.5 inhibitor with improved selectivity and pharmacokinetics.
Wolkenberg SE, Nolt MB, Bilodeau MT, Trotter BW, Manley PJ, Kett NR, Nanda KK, Wu Z, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Dinsmore CJ, Lindsley CW, Hartman GD. Wolkenberg SE, et al. Among authors: kiss l. Bioorg Med Chem Lett. 2017 Feb 15;27(4):1062-1069. doi: 10.1016/j.bmcl.2016.12.054. Epub 2017 Jan 16. Bioorg Med Chem Lett. 2017. PMID: 28131713
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Trotter BW, Nanda KK, Kett NR, Regan CP, Lynch JJ, Stump GL, Kiss L, Wang J, Spencer RH, Kane SA, White RB, Zhang R, Anderson KD, Liverton NJ, McIntyre CJ, Beshore DC, Hartman GD, Dinsmore CJ. Trotter BW, et al. Among authors: kiss l. J Med Chem. 2006 Nov 30;49(24):6954-7. doi: 10.1021/jm060927v. J Med Chem. 2006. PMID: 17125248
Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel.
Beshore DC, Liverton NJ, McIntyre CJ, Claiborne CF, Libby B, Culberson JC, Salata JJ, Regan CP, Lynch JJ, Kiss L, Spencer RH, Kane SA, White RB, Yeh S, Hartman GD, Dinsmore CJ. Beshore DC, et al. Among authors: kiss l. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2493-6. doi: 10.1016/j.bmcl.2010.03.005. Epub 2010 Mar 4. Bioorg Med Chem Lett. 2010. PMID: 20304642
Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.
Nanda KK, Nolt MB, Cato MJ, Kane SA, Kiss L, Spencer RH, Wang J, Lynch JJ, Regan CP, Stump GL, Li B, White R, Yeh S, Bogusky MJ, Bilodeau MT, Dinsmore CJ, Lindsley CW, Hartman GD, Wolkenberg SE, Trotter BW. Nanda KK, et al. Among authors: kiss l. Bioorg Med Chem Lett. 2006 Nov 15;16(22):5897-901. doi: 10.1016/j.bmcl.2006.08.054. Epub 2006 Sep 1. Bioorg Med Chem Lett. 2006. PMID: 16949818
749 results