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Items: 1 to 20 of 146

1.

Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).

Hu E, Kunz RK, Chen N, Rumfelt S, Siegmund A, Andrews K, Chmait S, Zhao S, Davis C, Chen H, Lester-Zeiner D, Ma J, Biorn C, Shi J, Porter A, Treanor J, Allen JR.

J Med Chem. 2013 Nov 14;56(21):8781-92. doi: 10.1021/jm401234w. Epub 2013 Oct 25.

PMID:
24102193
2.

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
3.

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
4.

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
5.

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Hu E, Chen N, Bourbeau MP, Harrington PE, Biswas K, Kunz RK, Andrews KL, Chmait S, Zhao X, Davis C, Ma J, Shi J, Lester-Zeiner D, Danao J, Able J, Cueva M, Talreja S, Kornecook T, Chen H, Porter A, Hungate R, Treanor J, Allen JR.

J Med Chem. 2014 Aug 14;57(15):6632-41. doi: 10.1021/jm500713j. Epub 2014 Aug 4.

PMID:
25062128
6.

Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.

Hu E, Kunz RK, Rumfelt S, Chen N, Bürli R, Li C, Andrews KL, Zhang J, Chmait S, Kogan J, Lindstrom M, Hitchcock SA, Treanor J.

Bioorg Med Chem Lett. 2012 Mar 15;22(6):2262-5. doi: 10.1016/j.bmcl.2012.01.086. Epub 2012 Feb 8.

PMID:
22365755
7.

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
8.

AMG 580: a novel small molecule phosphodiesterase 10A (PDE10A) positron emission tomography tracer.

Chen H, Lester-Zeiner D, Shi J, Miller S, Glaus C, Hu E, Chen N, Able J, Biorn C, Wong J, Ma J, Michelsen K, Hill Della Puppa G, Kazules T, Dou HH, Talreja S, Zhao X, Chen A, Rumfelt S, Kunz RK, Ye H, Thiel OR, Williamson T, Davis C, Porter A, Immke D, Allen JR, Treanor J.

J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. doi: 10.1124/jpet.114.220517. Epub 2014 Dec 11.

9.

Novel triazines as potent and selective phosphodiesterase 10A inhibitors.

Malamas MS, Stange H, Schindler R, Lankau HJ, Grunwald C, Langen B, Egerland U, Hage T, Ni Y, Erdei J, Fan KY, Parris K, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Brandon NJ, Hoefgen N.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5876-84. doi: 10.1016/j.bmcl.2012.07.076. Epub 2012 Jul 31.

PMID:
22902656
10.

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
11.

Rapid identification of a novel small molecule phosphodiesterase 10A (PDE10A) tracer.

Hu E, Ma J, Biorn C, Lester-Zeiner D, Cho R, Rumfelt S, Kunz RK, Nixey T, Michelsen K, Miller S, Shi J, Wong J, Hill Della Puppa G, Able J, Talreja S, Hwang DR, Hitchcock SA, Porter A, Immke D, Allen JR, Treanor J, Chen H.

J Med Chem. 2012 May 24;55(10):4776-87. doi: 10.1021/jm3002372. Epub 2012 May 11.

PMID:
22548439
12.

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
13.

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
14.

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
15.

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
16.

Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: part II.

Das S, Shelke DE, Harde RL, Avhad VB, Khairatkar-Joshi N, Gullapalli S, Gupta PK, Gandhi MN, Bhateja DK, Bajpai M, Joshi AA, Marathe MY, Gudi GS, Jadhav SB, Mahat MY, Thomas A.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3238-42. doi: 10.1016/j.bmcl.2014.06.028. Epub 2014 Jun 19.

PMID:
24980052
17.

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors.

Malamas MS, Ni Y, Erdei J, Stange H, Schindler R, Lankau HJ, Grunwald C, Fan KY, Parris K, Langen B, Egerland U, Hage T, Marquis KL, Grauer S, Brennan J, Navarra R, Graf R, Harrison BL, Robichaud A, Kronbach T, Pangalos MN, Hoefgen N, Brandon NJ.

J Med Chem. 2011 Nov 10;54(21):7621-38. doi: 10.1021/jm2009138. Epub 2011 Oct 11.

PMID:
21988093
18.

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
19.

Design, synthesis and pharmacological evaluation of novel polycyclic heteroarene ethers as PDE10A inhibitors: Part I.

Das S, Harde RL, Shelke DE, Khairatkar-Joshi N, Bajpai M, Sapalya RS, Surve HV, Gudi GS, Pattem R, Behera DB, Jadhav SB, Thomas A.

Bioorg Med Chem Lett. 2014 May 1;24(9):2073-8. doi: 10.1016/j.bmcl.2014.03.054. Epub 2014 Mar 28.

PMID:
24725435
20.

Synthesis and in vitro characterization of cinnoline and benzimidazole analogues as phosphodiesterase 10A inhibitors.

Yang H, Murigi FN, Wang Z, Li J, Jin H, Tu Z.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):919-24. doi: 10.1016/j.bmcl.2014.12.054. Epub 2014 Dec 22.

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