Kokubo M - Search Results

1

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW. Gentry PR, et al. Among authors: kokubo m. J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13. J Med Chem. 2013. PMID: 24164599 Free PMC article.

2

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.

Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW. Gentry PR, et al. Among authors: kokubo m. ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1. ChemMedChem. 2014. PMID: 24692176 Free PMC article.

3

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR. Gentry PR, et al. Among authors: kokubo m. J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3. J Med Chem. 2014. PMID: 25147929 Free PMC article.

4

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

Kurata H, Gentry PR, Kokubo M, Cho HP, Bridges TM, Niswender CM, Byers FW, Wood MR, Daniels JS, Conn PJ, Lindsley CW. Kurata H, et al. Among authors: kokubo m. Bioorg Med Chem Lett. 2015 Feb 1;25(3):690-4. doi: 10.1016/j.bmcl.2014.11.082. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25542588 Free PMC article.

5

Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249.

Iwaki Y, Yashiro K, Kokubo M, Mori T, Wieting JM, McGowan KM, Bridges TM, Engers DW, Denton JS, Kurata H, Lindsley CW. Iwaki Y, et al. Among authors: kokubo m. Bioorg Med Chem Lett. 2019 Jul 1;29(13):1601-1604. doi: 10.1016/j.bmcl.2019.04.048. Epub 2019 Apr 29. Bioorg Med Chem Lett. 2019. PMID: 31072652

6

Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.

Habashita H, Kokubo M, Hamano S, Hamanaka N, Toda M, Shibayama S, Tada H, Sagawa K, Fukushima D, Maeda K, Mitsuya H. Habashita H, et al. Among authors: kokubo m. J Med Chem. 2006 Jul 13;49(14):4140-52. doi: 10.1021/jm060051s. J Med Chem. 2006. PMID: 16821774

7

Suppressive effects of a novel CC chemokine receptor 4 antagonist on Th2 cell trafficking in ligand- and antigen-induced mouse models.

Komiya T, Sugiyama T, Takeda K, Watanabe N, Imai M, Kokubo M, Tokuda N, Ochiai H, Habashita H, Shibayama S. Komiya T, et al. Among authors: kokubo m. Eur J Pharmacol. 2013 Nov 15;720(1-3):335-43. doi: 10.1016/j.ejphar.2013.10.006. Epub 2013 Oct 16. Eur J Pharmacol. 2013. PMID: 24140571

8

Chiral scandium-catalyzed enantioselective hydroxymethylation of ketones in water.

Kobayashi S, Kokubo M, Kawasumi K, Nagano T. Kobayashi S, et al. Among authors: kokubo m. Chem Asian J. 2010 Mar 1;5(3):490-2. doi: 10.1002/asia.200900442. Chem Asian J. 2010. PMID: 20063342 No abstract available.

9

Lewis acid catalysis in water with a hydrophilic substrate: scandium-catalyzed hydroxymethylation with aqueous formaldehyde in water.

Kokubo M, Ogawa C, Kobayashi S. Kokubo M, et al. Angew Chem Int Ed Engl. 2008;47(36):6909-11. doi: 10.1002/anie.200801849. Angew Chem Int Ed Engl. 2008. PMID: 18666189 No abstract available.

10

Nazarov-type reactions in water.

Kokubo M, Kobayashi S. Kokubo M, et al. Chem Asian J. 2009 Apr 6;4(4):526-8. doi: 10.1002/asia.200800461. Chem Asian J. 2009. PMID: 19212964

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