Detalhe da pesquisa
1.
Positive allosteric modulators (PAMs) of the group II metabotropic glutamate receptors: Design, synthesis, and evaluation as ex-vivo tool compounds.
Bioorg Med Chem Lett
; 50: 128342, 2021 10 15.
Artigo
Inglês
| MEDLINE | ID: mdl-34461178
2.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 4: SAR reveals positive cooperativity across multiple mGlu receptor subtypes leading to subtype unselective PAMs.
Bioorg Med Chem Lett
; 32: 127724, 2021 01 15.
Artigo
Inglês
| MEDLINE | ID: mdl-33253881
3.
Novel M4 positive allosteric modulators derived from questioning the role and impact of a presumed intramolecular hydrogen-bonding motif in ß-amino carboxamide-harboring ligands.
Bioorg Med Chem Lett
; 29(3): 362-366, 2019 02 01.
Artigo
Inglês
| MEDLINE | ID: mdl-30580918
4.
VU6005806/AZN-00016130, an advanced M4 positive allosteric modulator (PAM) profiled as a potential preclinical development candidate.
Bioorg Med Chem Lett
; 29(14): 1714-1718, 2019 07 15.
Artigo
Inglês
| MEDLINE | ID: mdl-31113706
5.
SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M4 PAMs.
Bioorg Med Chem Lett
; 29(16): 2224-2228, 2019 08 15.
Artigo
Inglês
| MEDLINE | ID: mdl-31248774
6.
Structural insights into HDAC6 tubulin deacetylation and its selective inhibition.
Nat Chem Biol
; 12(9): 748-54, 2016 09.
Artigo
Inglês
| MEDLINE | ID: mdl-27454931
7.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Bioorg Med Chem Lett
; 27(23): 5179-5184, 2017 12 01.
Artigo
Inglês
| MEDLINE | ID: mdl-29089231
8.
Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs.
Bioorg Med Chem Lett
; 27(2): 171-175, 2017 01 15.
Artigo
Inglês
| MEDLINE | ID: mdl-27939174
9.
Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology.
Bioorg Med Chem Lett
; 27(11): 2296-2301, 2017 06 01.
Artigo
Inglês
| MEDLINE | ID: mdl-28442253
10.
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Bioorg Med Chem Lett
; 26(13): 3029-3033, 2016 07 01.
Artigo
Inglês
| MEDLINE | ID: mdl-27185330
11.
A concise Diels-Alder strategy leading to congeners of the ABC ring system of the marine alkaloid 'upenamide.
Tetrahedron Lett
; 57(30): 3252-3253, 2016 Jul 27.
Artigo
Inglês
| MEDLINE | ID: mdl-33828342
12.
Microplate-based assay for identifying small molecules that bind a specific intersubunit interface within the assembled HIV-1 capsid.
Antimicrob Agents Chemother
; 59(9): 5190-5, 2015 Sep.
Artigo
Inglês
| MEDLINE | ID: mdl-26077250
13.
Substituted indoles as selective protease activated receptor 4 (PAR-4) antagonists: Discovery and SAR of ML354.
Bioorg Med Chem Lett
; 24(19): 4708-4713, 2014 Oct 01.
Artigo
Inglês
| MEDLINE | ID: mdl-25176330
14.
A structural model for binding of the serine-rich repeat adhesin GspB to host carbohydrate receptors.
PLoS Pathog
; 7(7): e1002112, 2011 Jul.
Artigo
Inglês
| MEDLINE | ID: mdl-21765814
15.
Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.
Bioorg Med Chem Lett
; 23(6): 1860-4, 2013 Mar 15.
Artigo
Inglês
| MEDLINE | ID: mdl-23416001
16.
Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.
Bioorg Med Chem Lett
; 23(2): 412-6, 2013 Jan 15.
Artigo
Inglês
| MEDLINE | ID: mdl-23237839
17.
Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia.
Bioorg Med Chem Lett
; 23(1): 346-50, 2013 Jan 01.
Artigo
Inglês
| MEDLINE | ID: mdl-23177787
18.
Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184].
Bioorg Med Chem Lett
; 28(17): 3014, 2018 09 15.
Artigo
Inglês
| MEDLINE | ID: mdl-30076050
19.
Structural basis of allosteric modulation of metabotropic glutamate receptor activation and desensitization.
bioRxiv
; 2023 Aug 14.
Artigo
Inglês
| MEDLINE | ID: mdl-37645747
20.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Bioorg Med Chem Lett
; 22(2): 1044-8, 2012 Jan 15.
Artigo
Inglês
| MEDLINE | ID: mdl-22197142