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Items: 1 to 20 of 110

1.

N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors.

Kilburn JP, Kehler J, Langgård M, Erichsen MN, Leth-Petersen S, Larsen M, Christoffersen CT, Nielsen J.

Bioorg Med Chem. 2013 Oct 1;21(19):6053-62. doi: 10.1016/j.bmc.2013.07.030. Epub 2013 Jul 23.

PMID:
23978358
2.

Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.

Kehler J, Ritzen A, Langgård M, Petersen SL, Farah MM, Bundgaard C, Christoffersen CT, Nielsen J, Kilburn JP.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3738-42. doi: 10.1016/j.bmcl.2011.04.067. Epub 2011 Apr 30.

PMID:
21602043
3.

Discovery of [¹¹C]MK-8193 as a PET tracer to measure target engagement of phosphodiesterase 10A (PDE10A) inhibitors.

Cox CD, Hostetler ED, Flores BA, Evelhoch JL, Fan H, Gantert L, Holahan M, Eng W, Joshi A, McGaughey G, Meng X, Purcell M, Raheem IT, Riffel K, Yan Y, Renger JJ, Smith SM, Coleman PJ.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4893-8. doi: 10.1016/j.bmcl.2015.05.080. Epub 2015 Jun 1.

PMID:
26077491
4.

Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition.

Hamaguchi W, Masuda N, Isomura M, Miyamoto S, Kikuchi S, Amano Y, Honbou K, Mihara T, Watanabe T.

Bioorg Med Chem. 2013 Dec 15;21(24):7612-23. doi: 10.1016/j.bmc.2013.10.035. Epub 2013 Oct 31.

PMID:
24238902
5.

BN/CC isosterism in borazaronaphthalenes towards phosphodiesterase 10A (PDE10A) inhibitors.

Vlasceanu A, Jessing M, Kilburn JP.

Bioorg Med Chem. 2015 Aug 1;23(15):4453-61. doi: 10.1016/j.bmc.2015.06.019. Epub 2015 Jun 15.

PMID:
26113188
6.

Novel benzimidazole derivatives as phosphodiesterase 10A (PDE10A) inhibitors with improved metabolic stability.

Chino A, Masuda N, Amano Y, Honbou K, Mihara T, Yamazaki M, Tomishima M.

Bioorg Med Chem. 2014 Jul 1;22(13):3515-26. doi: 10.1016/j.bmc.2014.04.023. Epub 2014 Apr 20.

PMID:
24837154
7.

Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.

Yoshikawa M, Kamisaki H, Kunitomo J, Oki H, Kokubo H, Suzuki A, Ikemoto T, Nakashima K, Kamiguchi N, Harada A, Kimura H, Taniguchi T.

Bioorg Med Chem. 2015 Nov 15;23(22):7138-49. doi: 10.1016/j.bmc.2015.10.002. Epub 2015 Oct 9.

PMID:
26494583
8.

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.

Bioorg Med Chem Lett. 2016 Jan 1;26(1):126-32. doi: 10.1016/j.bmcl.2015.11.013. Epub 2015 Nov 10.

PMID:
26602277
9.

Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis.

Shipe WD, Sharik SS, Barrow JC, McGaughey GB, Theberge CR, Uslaner JM, Yan Y, Renger JJ, Smith SM, Coleman PJ, Cox CD.

J Med Chem. 2015 Oct 8;58(19):7888-94. doi: 10.1021/acs.jmedchem.5b00983. Epub 2015 Sep 25.

PMID:
26378882
10.

Discovery of a series of 6,7-dimethoxy-4-pyrrolidylquinazoline PDE10A inhibitors.

Chappie TA, Humphrey JM, Allen MP, Estep KG, Fox CB, Lebel LA, Liras S, Marr ES, Menniti FS, Pandit J, Schmidt CJ, Tu M, Williams RD, Yang FV.

J Med Chem. 2007 Jan 25;50(2):182-5.

PMID:
17228859
11.

Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.

Asproni B, Murineddu G, Pau A, Pinna GA, Langgård M, Christoffersen CT, Nielsen J, Kehler J.

Bioorg Med Chem. 2011 Jan 1;19(1):642-9. doi: 10.1016/j.bmc.2010.10.038. Epub 2010 Nov 17.

PMID:
21087867
12.

Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

Rzasa RM, Hu E, Rumfelt S, Chen N, Andrews KL, Chmait S, Falsey JR, Zhong W, Jones AD, Porter A, Louie SW, Zhao X, Treanor JJ, Allen JR.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7371-5. doi: 10.1016/j.bmcl.2012.10.078. Epub 2012 Oct 22.

PMID:
23149228
13.

Identification of a novel orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor with efficacy in animal models of schizophrenia.

Bartolomé-Nebreda JM, Alonso de Diego SA, Artola M, Delgado F, Delgado Ó, Martín-Martín ML, Martínez-Viturro CM, Pena MÁ, Tong HM, Van Gool M, Alonso JM, Fontana A, Macdonald GJ, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S.

J Med Chem. 2015 Jan 22;58(2):978-93. doi: 10.1021/jm501651a. Epub 2015 Jan 12.

PMID:
25495129
14.

Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A.

Zhang Z, Lu X, Xu J, Rothfuss J, Mach RH, Tu Z.

Eur J Med Chem. 2011 Sep;46(9):3986-95. doi: 10.1016/j.ejmech.2011.05.072. Epub 2011 Jun 12.

15.

Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.

Wagner S, Scheunemann M, Dipper K, Egerland U, Hoefgen N, Steinbach J, Brust P.

Eur J Med Chem. 2016 Jan 1;107:97-108. doi: 10.1016/j.ejmech.2015.10.028. Epub 2015 Oct 19.

PMID:
26562545
16.

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.

Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJ, Allen JR.

Bioorg Med Chem. 2014 Dec 1;22(23):6570-85.

PMID:
25456383
17.

Synthesis, SAR study, and biological evaluation of novel quinoline derivatives as phosphodiesterase 10A inhibitors with reduced CYP3A4 inhibition.

Hamaguchi W, Masuda N, Miyamoto S, Shiina Y, Kikuchi S, Mihara T, Moriguchi H, Fushiki H, Murakami Y, Amano Y, Honbou K, Hattori K.

Bioorg Med Chem. 2015 Jan 15;23(2):297-313. doi: 10.1016/j.bmc.2014.11.039. Epub 2014 Dec 3.

PMID:
25515954
18.

Discovery of 4-hydroxy-1,6-naphthyridine-3-carbonitrile derivatives as novel PDE10A inhibitors.

Bauer U, Giordanetto F, Bauer M, O'Mahony G, Johansson KE, Knecht W, Hartleib-Geschwindner J, Carlsson ET, Enroth C.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1944-8. doi: 10.1016/j.bmcl.2012.01.046. Epub 2012 Jan 26.

PMID:
22321214
19.

Discovery of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.

Bartolomé-Nebreda JM, Delgado F, Martín-Martín ML, Martínez-Viturro CM, Pastor J, Tong HM, Iturrino L, Macdonald GJ, Sanderson W, Megens A, Langlois X, Somers M, Vanhoof G, Conde-Ceide S.

J Med Chem. 2014 May 22;57(10):4196-212. doi: 10.1021/jm500073h. Epub 2014 May 9.

PMID:
24758746
20.

Synthesis and SAR study of novel tricyclic pyrazoles as potent phosphodiesterase 10A inhibitors.

Dore A, Asproni B, Scampuddu A, Pinna GA, Christoffersen CT, Langgård M, Kehler J.

Eur J Med Chem. 2014 Sep 12;84:181-93. doi: 10.1016/j.ejmech.2014.07.020. Epub 2014 Jul 7.

PMID:
25016376

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