These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.
5. Discovery of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid β-peptides. Rueeger H; Lueoend R; Rogel O; Rondeau JM; Möbitz H; Machauer R; Jacobson L; Staufenbiel M; Desrayaud S; Neumann U J Med Chem; 2012 Apr; 55(7):3364-86. PubMed ID: 22380629 [TBL] [Abstract][Full Text] [Related]
6. Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors. Volgraf M; Chan L; Huestis MP; Purkey HE; Burkard M; Geck Do M; Harris J; Hunt KW; Liu X; Lyssikatos JP; Rana S; Thomas AA; Vigers GP; Siu M Bioorg Med Chem Lett; 2014 Jun; 24(11):2477-80. PubMed ID: 24780121 [TBL] [Abstract][Full Text] [Related]
7. Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Epstein O; Bryan MC; Cheng AC; Derakhchan K; Dineen TA; Hickman D; Hua Z; Human JB; Kreiman C; Marx IE; Weiss MM; Wahl RC; Wen PH; Whittington DA; Wood S; Zheng XM; Fremeau RT; White RD; Patel VF J Med Chem; 2014 Dec; 57(23):9796-810. PubMed ID: 25389560 [TBL] [Abstract][Full Text] [Related]
8. Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors. Dineen TA; Weiss MM; Williamson T; Acton P; Babu-Khan S; Bartberger MD; Brown J; Chen K; Cheng Y; Citron M; Croghan MD; Dunn RT; Esmay J; Graceffa RF; Harried SS; Hickman D; Hitchcock SA; Horne DB; Huang H; Imbeah-Ampiah R; Judd T; Kaller MR; Kreiman CR; La DS; Li V; Lopez P; Louie S; Monenschein H; Nguyen TT; Pennington LD; San Miguel T; Sickmier EA; Vargas HM; Wahl RC; Wen PH; Whittington DA; Wood S; Xue Q; Yang BH; Patel VF; Zhong W J Med Chem; 2012 Nov; 55(21):9025-44. PubMed ID: 22468684 [TBL] [Abstract][Full Text] [Related]
9. From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1). Cheng Y; Judd TC; Bartberger MD; Brown J; Chen K; Fremeau RT; Hickman D; Hitchcock SA; Jordan B; Li V; Lopez P; Louie SW; Luo Y; Michelsen K; Nixey T; Powers TS; Rattan C; Sickmier EA; St Jean DJ; Wahl RC; Wen PH; Wood S J Med Chem; 2011 Aug; 54(16):5836-57. PubMed ID: 21707077 [TBL] [Abstract][Full Text] [Related]
10. P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice. Meredith JE; Thompson LA; Toyn JH; Marcin L; Barten DM; Marcinkeviciene J; Kopcho L; Kim Y; Lin A; Guss V; Burton C; Iben L; Polson C; Cantone J; Ford M; Drexler D; Fiedler T; Lentz KA; Grace JE; Kolb J; Corsa J; Pierdomenico M; Jones K; Olson RE; Macor JE; Albright CF J Pharmacol Exp Ther; 2008 Aug; 326(2):502-13. PubMed ID: 18499745 [TBL] [Abstract][Full Text] [Related]
11. Discovery of pyrazole as C-terminus of selective BACE1 inhibitors. Zou Y; Xu L; Chen W; Zhu Y; Chen T; Fu Y; Li L; Ma L; Xiong B; Wang X; Li J; He J; Zhang H; Xu Y; Li J; Shen J Eur J Med Chem; 2013 Oct; 68():270-83. PubMed ID: 23988410 [TBL] [Abstract][Full Text] [Related]
12. New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region. Malamas MS; Erdei J; Gunawan I; Barnes K; Hui Y; Johnson M; Robichaud A; Zhou P; Yan Y; Solvibile W; Turner J; Fan KY; Chopra R; Bard J; Pangalos MN Bioorg Med Chem Lett; 2011 Sep; 21(18):5164-70. PubMed ID: 21835615 [TBL] [Abstract][Full Text] [Related]
13. Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors. Ng RA; Sun M; Bowers S; Hom RK; Probst GD; John V; Fang LY; Maillard M; Gailunas A; Brogley L; Neitz RJ; Tung JS; Pleiss MA; Konradi AW; Sham HL; Dappen MS; Adler M; Yao N; Zmolek W; Nakamura D; Quinn KP; Sauer JM; Bova MP; Ruslim L; Artis DR; Yednock TA Bioorg Med Chem Lett; 2013 Aug; 23(16):4674-9. PubMed ID: 23856050 [TBL] [Abstract][Full Text] [Related]
14. Hydroxyethylamine-based inhibitors of BACE1: P₁-P₃ macrocyclization can improve potency, selectivity, and cell activity. Pennington LD; Whittington DA; Bartberger MD; Jordan SR; Monenschein H; Nguyen TT; Yang BH; Xue QM; Vounatsos F; Wahl RC; Chen K; Wood S; Citron M; Patel VF; Hitchcock SA; Zhong W Bioorg Med Chem Lett; 2013 Aug; 23(15):4459-64. PubMed ID: 23769639 [TBL] [Abstract][Full Text] [Related]
15. Mechanistic pharmacokinetic-pharmacodynamic modeling of BACE1 inhibition in monkeys: development of a predictive model for amyloid precursor protein processing. Liu X; Wong H; Scearce-Levie K; Watts RJ; Coraggio M; Shin YG; Peng K; Wildsmith KR; Atwal JK; Mango J; Schauer SP; Regal K; Hunt KW; Thomas AA; Siu M; Lyssikatos J; Deshmukh G; Hop CE Drug Metab Dispos; 2013 Jul; 41(7):1319-28. PubMed ID: 23584887 [TBL] [Abstract][Full Text] [Related]
16. Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors. Brodney MA; Barreiro G; Ogilvie K; Hajos-Korcsok E; Murray J; Vajdos F; Ambroise C; Christoffersen C; Fisher K; Lanyon L; Liu J; Nolan CE; Withka JM; Borzilleri KA; Efremov I; Oborski CE; Varghese A; O'Neill BT J Med Chem; 2012 Nov; 55(21):9224-39. PubMed ID: 22984865 [TBL] [Abstract][Full Text] [Related]
18. The selective BACE1 inhibitor VIa reduces amyloid-β production in cell and mouse models of Alzheimer's disease. Cheng X; Zhou Y; Gu W; Wu J; Nie A; Cheng J; Zhou J; Zhou W; Zhang Y J Alzheimers Dis; 2013; 37(4):823-34. PubMed ID: 23948917 [TBL] [Abstract][Full Text] [Related]
19. Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities. De Tran Q; Bepary S; Lee GH; Cho H; Park WK; Lim HJ Bioorg Med Chem Lett; 2016 Jan; 26(1):51-4. PubMed ID: 26608551 [TBL] [Abstract][Full Text] [Related]
20. Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors. Malamas MS; Erdei J; Gunawan I; Barnes K; Johnson M; Hui Y; Turner J; Hu Y; Wagner E; Fan K; Olland A; Bard J; Robichaud AJ J Med Chem; 2009 Oct; 52(20):6314-23. PubMed ID: 19757823 [TBL] [Abstract][Full Text] [Related] [Next] [New Search]