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Page 1
Pyrazole Ureas as Low Dose, CNS Penetrant Glucosylceramide Synthase Inhibitors for the Treatment of Parkinson's Disease.
Roecker AJ, Schirripa KM, Loughran HM, Tong L, Liang T, Fillgrove KL, Kuo Y, Bleasby K, Collier H, Altman MD, Ford MC, Drolet RE, Cosden M, Jinn S, Hatcher NG, Yao L, Kandebo M, Vardigan JD, Flick RB, Liu X, Minnick C, Price LA, Watt ML, Lemaire W, Burlein C, Adam GC, Austin LA, Marcus JN, Smith SM, Fraley ME. Roecker AJ, et al. Among authors: kandebo m. ACS Med Chem Lett. 2023 Jan 12;14(2):146-155. doi: 10.1021/acsmedchemlett.2c00441. eCollection 2023 Feb 9. ACS Med Chem Lett. 2023. PMID: 36793422 Free PMC article.
The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.
Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ. Smith SM, et al. Among authors: kandebo m. Neuropharmacology. 2013 Jan;64:215-23. doi: 10.1016/j.neuropharm.2012.06.013. Epub 2012 Jun 27. Neuropharmacology. 2013. PMID: 22750078
Characterization of non-nitrocatechol pan and isoform specific catechol-O-methyltransferase inhibitors and substrates.
Robinson RG, Smith SM, Wolkenberg SE, Kandebo M, Yao L, Gibson CR, Harrison ST, Polsky-Fisher S, Barrow JC, Manley PJ, Mulhearn JJ, Nanda KK, Schubert JW, Trotter BW, Zhao Z, Sanders JM, Smith RF, McLoughlin D, Sharma S, Hall DL, Walker TL, Kershner JL, Bhandari N, Hutson PH, Sachs NA. Robinson RG, et al. Among authors: kandebo m. ACS Chem Neurosci. 2012 Feb 15;3(2):129-40. doi: 10.1021/cn200109w. Epub 2011 Nov 14. ACS Chem Neurosci. 2012. PMID: 22860182 Free PMC article.
Discovery of tetrahydropyridopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Raheem IT, Breslin MJ, Fandozzi C, Fuerst J, Hill N, Huszar S, Kandebo M, Kim SH, Ma B, McGaughey G, Renger JJ, Schreier JD, Sharma S, Smith S, Uslaner J, Yan Y, Coleman PJ, Cox CD. Raheem IT, et al. Among authors: kandebo m. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5903-8. doi: 10.1016/j.bmcl.2012.07.072. Epub 2012 Jul 27. Bioorg Med Chem Lett. 2012. PMID: 22892116
Discovery of pyrazolopyrimidine phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Raheem IT, Schreier JD, Fuerst J, Gantert L, Hostetler ED, Huszar S, Joshi A, Kandebo M, Kim SH, Li J, Ma B, McGaughey G, Sharma S, Shipe WD, Uslaner J, Vandeveer GH, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD. Raheem IT, et al. Among authors: kandebo m. Bioorg Med Chem Lett. 2016 Jan 1;26(1):126-32. doi: 10.1016/j.bmcl.2015.11.013. Epub 2015 Nov 10. Bioorg Med Chem Lett. 2016. PMID: 26602277
Synthesis and optimization of N-heterocyclic pyridinones as catechol-O-methyltransferase (COMT) inhibitors.
Zhao Z, Harrison ST, Schubert JW, Sanders JM, Polsky-Fisher S, Zhang NR, McLoughlin D, Gibson CR, Robinson RG, Sachs NA, Kandebo M, Yao L, Smith SM, Hutson PH, Wolkenberg SE, Barrow JC. Zhao Z, et al. Among authors: kandebo m. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2952-2956. doi: 10.1016/j.bmcl.2016.03.095. Epub 2016 Apr 7. Bioorg Med Chem Lett. 2016. PMID: 27133481
Decreased glucocerebrosidase activity and substrate accumulation of glycosphingolipids in a novel GBA1 D409V knock-in mouse model.
Polinski NK, Martinez TN, Gorodinsky A, Gareus R, Sasner M, Herberth M, Switzer R, Ahmad SO, Cosden M, Kandebo M, Drolet RE, Buckett PD, Shan W, Chen Y, Pellegrino LJ, Ellsworth GD, Dungan LB, Hirst WD, Clark SW, Dave KD. Polinski NK, et al. Among authors: kandebo m. PLoS One. 2021 Jun 9;16(6):e0252325. doi: 10.1371/journal.pone.0252325. eCollection 2021. PLoS One. 2021. PMID: 34106956 Free PMC article.
A novel glucosylceramide synthase inhibitor attenuates alpha synuclein pathology and lysosomal dysfunction in preclinical models of synucleinopathy.
Cosden M, Jinn S, Yao L, Gretzula CA, Kandebo M, Toolan D, Hatcher NG, Ma L, Lemaire W, Adam GC, Burlein C, Minnick C, Flick R, Watt ML, Mulhearn J, Fraley M, Drolet RE, Marcus JN, Smith SM. Cosden M, et al. Among authors: kandebo m. Neurobiol Dis. 2021 Nov;159:105507. doi: 10.1016/j.nbd.2021.105507. Epub 2021 Sep 9. Neurobiol Dis. 2021. PMID: 34509608 Free article.
Discovery of MK-8189, a Highly Potent and Selective PDE10A Inhibitor for the Treatment of Schizophrenia.
Layton ME, Kern JC, Hartingh TJ, Shipe WD, Raheem I, Kandebo M, Hayes RP, Huszar S, Eddins D, Ma B, Fuerst J, Wollenberg GK, Li J, Fritzen J, McGaughey GB, Uslaner JM, Smith SM, Coleman PJ, Cox CD. Layton ME, et al. Among authors: kandebo m. J Med Chem. 2023 Jan 26;66(2):1157-1171. doi: 10.1021/acs.jmedchem.2c01521. Epub 2023 Jan 9. J Med Chem. 2023. PMID: 36624931 Free PMC article.
14 results