Detalhe da pesquisa
1.
Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902.
Endocrinology
; 148(2): 857-67, 2007 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-17095587
2.
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
J Med Chem
; 49(2): 637-47, 2006 Jan 26.
Artigo
em Inglês
| MEDLINE | ID: mdl-16420049
3.
Determination of the binding mode of thienopyrimidinedione antagonists to the human gonadotropin releasing hormone receptor using structure-activity relationships, site-directed mutagenesis, and homology modeling.
J Med Chem
; 49(21): 6170-6, 2006 Oct 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-17034124
4.
3-[(2R)-Amino-2-phenylethyl]-1-(2,6-difluorobenzyl)-5-(2-fluoro-3-methoxyphenyl)- 6-methylpyrimidin-2,4-dione (NBI 42902) as a potent and orally active antagonist of the human gonadotropin-releasing hormone receptor. Design, synthesis, and in vitro and in vivo characterization.
J Med Chem
; 48(4): 1169-78, 2005 Feb 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-15715483
5.
Design and structure-activity relationships of 2-alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
J Med Chem
; 46(9): 1769-72, 2003 Apr 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-12699396
6.
Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
J Med Chem
; 46(11): 2023-6, 2003 May 22.
Artigo
em Inglês
| MEDLINE | ID: mdl-12747774
7.
3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor.
J Med Chem
; 47(14): 3483-6, 2004 Jul 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-15214774
8.
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
J Med Chem
; 51(23): 7478-85, 2008 Dec 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-19006286
9.
Species selectivity of nonpeptide antagonists of the gonadotropin-releasing hormone receptor is determined by residues in extracellular loops II and III and the amino terminus.
J Biol Chem
; 279(33): 34115-22, 2004 Aug 13.
Artigo
em Inglês
| MEDLINE | ID: mdl-15155770
10.
Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists.
Bioorg Med Chem Lett
; 13(19): 3311-5, 2003 Oct 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-12951116
11.
Synthesis and structure-activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor.
Bioorg Med Chem Lett
; 13(19): 3317-22, 2003 Oct 06.
Artigo
em Inglês
| MEDLINE | ID: mdl-12951117
12.
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
Bioorg Med Chem Lett
; 12(3): 399-402, 2002 Feb 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-11814806
13.
Synthesis and initial structure-activity relationships of a novel series of imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Bioorg Med Chem Lett
; 12(16): 2179-83, 2002 Aug 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-12127532
14.
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Bioorg Med Chem Lett
; 14(9): 2269-74, 2004 May 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-15081023
15.
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.
Bioorg Med Chem Lett
; 12(23): 3491-5, 2002 Dec 02.
Artigo
em Inglês
| MEDLINE | ID: mdl-12419391
16.
A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.
Bioorg Med Chem Lett
; 12(3): 403-6, 2002 Feb 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-11814807
17.
Design, synthesis and structure-activity relationships of novel imidazolo[1,2-a]pyrimid-5-ones as potent GnRH receptor antagonists.
Bioorg Med Chem Lett
; 12(16): 2185-7, 2002 Aug 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-12127533