Detalles de la búsqueda
1.
A new brain-penetrant glucosylceramide synthase inhibitor as potential Therapeutics for Gaucher disease.
J Neurochem
; 159(3): 543-553, 2021 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-34398463
2.
Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders.
Chem Pharm Bull (Tokyo)
; 65(11): 1058-1077, 2017.
Artículo
en Inglés
| MEDLINE | ID: mdl-29093293
3.
Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket.
Bioorg Med Chem
; 24(16): 3447-55, 2016 08 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27301679
4.
Novel approach of fragment-based lead discovery applied to renin inhibitors.
Bioorg Med Chem
; 24(22): 6066-6074, 2016 11 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27720325
5.
Design, synthesis, and biological activity of novel, potent, and highly selective fused pyrimidine-2-carboxamide-4-one-based matrix metalloproteinase (MMP)-13 zinc-binding inhibitors.
Bioorg Med Chem
; 24(23): 6149-6165, 2016 12 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27825552
6.
Design and synthesis of a novel 2-oxindole scaffold as a highly potent and brain-penetrant phosphodiesterase 10A inhibitor.
Bioorg Med Chem
; 23(22): 7138-49, 2015 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26494583
7.
Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1â³ binding site.
Bioorg Med Chem
; 22(19): 5487-505, 2014 Oct 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-25192810
8.
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.
Bioorg Med Chem
; 21(1): 28-41, 2013 Jan 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-23218778
9.
Structure-based design, synthesis, and evaluation of imidazo[1,2-b]pyridazine and imidazo[1,2-a]pyridine derivatives as novel dual c-Met and VEGFR2 kinase inhibitors.
Bioorg Med Chem
; 21(24): 7686-98, 2013 Dec 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-24216091
10.
Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor.
Bioorg Med Chem
; 21(8): 2333-2345, 2013 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23498918
11.
Design, Synthesis, and Biological Evaluation of a Novel Series of 4-Guanidinobenzoate Derivatives as Enteropeptidase Inhibitors with Low Systemic Exposure for the Treatment of Obesity.
J Med Chem
; 65(12): 8456-8477, 2022 06 23.
Artículo
en Inglés
| MEDLINE | ID: mdl-35686954
12.
Design, synthesis, and structure-activity relationship of TAK-418 and its derivatives as a novel series of LSD1 inhibitors with lowered risk of hematological side effects.
Eur J Med Chem
; 239: 114522, 2022 Sep 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-35749987
13.
Discovery of Brain-Penetrant Glucosylceramide Synthase Inhibitors with a Novel Pharmacophore.
J Med Chem
; 65(5): 4270-4290, 2022 03 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-35188773
14.
Cryo-EM Structure of K+-Bound hERG Channel Complexed with the Blocker Astemizole.
Structure
; 29(3): 203-212.e4, 2021 03 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-33450182
15.
LSD1 enzyme inhibitor TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models.
Sci Adv
; 7(11)2021 03.
Artículo
en Inglés
| MEDLINE | ID: mdl-33712455
16.
T-448, a specific inhibitor of LSD1 enzyme activity, improves learning function without causing thrombocytopenia in mice.
Neuropsychopharmacology
; 44(8): 1505-1512, 2019 07.
Artículo
en Inglés
| MEDLINE | ID: mdl-30580376
17.
Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
J Med Chem
; 60(18): 7658-7676, 2017 09 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-28759228
18.
Discovery and Characterization of a Eukaryotic Initiation Factor 4A-3-Selective Inhibitor That Suppresses Nonsense-Mediated mRNA Decay.
ACS Chem Biol
; 12(7): 1760-1768, 2017 07 21.
Artículo
en Inglés
| MEDLINE | ID: mdl-28440616
19.
Discovery of a B-Cell Lymphoma 6 Protein-Protein Interaction Inhibitor by a Biophysics-Driven Fragment-Based Approach.
J Med Chem
; 60(10): 4358-4368, 2017 05 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-28471657
20.
Identification of cytidine-5-triphosphate synthase1-selective inhibitory peptide from random peptide library displayed on T7 phage.
Peptides
; 94: 56-63, 2017 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-28676225