Detalhe da pesquisa
1.
Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors.
Nature
; 504(7480): 437-40, 2013 Dec 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-24226772
2.
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Bioorg Med Chem
; 22(23): 6570-6585, 2014 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-25456383
3.
Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors.
Bioorg Med Chem Lett
; 22(6): 2262-5, 2012 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-22365755
4.
Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.
Bioorg Med Chem Lett
; 22(24): 7371-5, 2012 Dec 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23149228
5.
Identification of triazolopyridazinones as potent p38α inhibitors.
Bioorg Med Chem Lett
; 22(2): 1226-9, 2012 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-22196117
6.
Part 2: Structure-activity relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Bioorg Med Chem Lett
; 20(5): 1680-4, 2010 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-20138761
7.
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Bioorg Med Chem Lett
; 19(16): 4724-8, 2009 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19574047
8.
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.
J Med Chem
; 58(11): 4462-82, 2015 Jun 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-25914941
9.
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N â S (nN â σ*S-X) Interaction for Conformational Constraint.
J Med Chem
; 58(24): 9663-79, 2015 Dec 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-26551034
10.
Discovery of Novel Imidazo[4,5-b]pyridines as Potent and Selective Inhibitors of Phosphodiesterase 10A (PDE10A).
ACS Med Chem Lett
; 5(6): 700-5, 2014 Jun 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-24944747
11.
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.
J Med Chem
; 57(14): 5949-64, 2014 Jul 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-25001129
12.
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).
J Med Chem
; 57(15): 6632-41, 2014 Aug 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-25062128
13.
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.
J Med Chem
; 57(7): 3094-116, 2014 Apr 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-24611879
14.
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
J Med Chem
; 57(2): 309-24, 2014 Jan 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-24405172
15.
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
J Med Chem
; 57(2): 325-38, 2014 Jan 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-24405213
16.
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
J Med Chem
; 56(21): 8781-92, 2013 Nov 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-24102193
17.
Discovery and evaluation of 7-alkyl-1,5-bis-aryl-pyrazolopyridinones as highly potent, selective, and orally efficacious inhibitors of p38alpha mitogen-activated protein kinase.
J Med Chem
; 53(7): 2973-85, 2010 Apr 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-20218619