Detalhe da pesquisa
1.
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
Bioorg Med Chem Lett
; 29(14): 1842-1848, 2019 07 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31109791
2.
Discovery and development of benzo-[1,2,4]-triazolo-[1,4]-oxazepine GPR142 agonists for the treatment of diabetes.
Bioorg Med Chem Lett
; 26(12): 2947-2951, 2016 06 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27240550
3.
SAR exploration at the C-3 position of tetrahydro-ß-carboline sstr3 antagonists.
Bioorg Med Chem Lett
; 26(6): 1529-1535, 2016 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26898814
4.
Discovery of substituted (4-phenyl-1H-imidazol-2-yl)methanamine as potent somatostatin receptor 3 agonists.
Bioorg Med Chem Lett
; 25(17): 3520-5, 2015 Sep 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26199120
5.
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
J Med Chem
; 65(24): 16234-16251, 2022 12 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-36475645
6.
Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Bioorg Med Chem Lett
; 20(16): 4757-61, 2010 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-20643546
7.
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.
Bioorg Med Chem Lett
; 19(17): 5195-9, 2009 Sep 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19632830
8.
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
J Med Chem
; 51(7): 2108-14, 2008 Apr 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-18333607
9.
Characterization of a novel and selective cannabinoid CB1 receptor inverse agonist, Imidazole 24b, in rodents.
Eur J Pharmacol
; 579(1-3): 215-24, 2008 Jan 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-18021763
10.
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Bioorg Med Chem Lett
; 18(5): 1688-91, 2008 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-18242984
11.
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.
J Med Chem
; 50(15): 3427-30, 2007 Jul 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-17608398
12.
GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production.
PLoS One
; 12(5): e0176182, 2017.
Artigo
em Inglês
| MEDLINE | ID: mdl-28542610
13.
Design and Synthesis of Novel, Selective GPR40 AgoPAMs.
ACS Med Chem Lett
; 8(2): 221-226, 2017 Feb 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-28197316
14.
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.
J Med Chem
; 49(26): 7584-7, 2006 Dec 28.
Artigo
em Inglês
| MEDLINE | ID: mdl-17181138
15.
F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist.
Eur J Pharmacol
; 531(1-3): 41-6, 2006 Feb 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-16438957
16.
Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.
ACS Med Chem Lett
; 7(12): 1107-1111, 2016 Dec 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-27994747
17.
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
ACS Med Chem Lett
; 6(5): 513-7, 2015 May 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-26005524
18.
The discovery and potential of N-sulfonylated dipeptide VLA-4 antagonists.
Curr Top Med Chem
; 4(14): 1461-71, 2004.
Artigo
em Inglês
| MEDLINE | ID: mdl-15544537
19.
Addressing the metabolic activation potential of new leads in drug discovery: a case study using ion trap mass spectrometry and tritium labeling techniques.
J Mass Spectrom
; 38(2): 211-21, 2003 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-12577288
20.
Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.
ACS Med Chem Lett
; 5(6): 690-5, 2014 Jun 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-24944745