Detalhe da pesquisa
1.
Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.
Bioorg Med Chem Lett
; 87: 129256, 2023 05 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-36966977
2.
Discovery of a potent M5 antagonist with improved clearance profile. Part 2: Pyrrolidine amide-based antagonists.
Bioorg Med Chem Lett
; 78: 129021, 2022 12 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-36228968
3.
Activation of the mGlu1 metabotropic glutamate receptor has antipsychotic-like effects and is required for efficacy of M4 muscarinic receptor allosteric modulators.
Mol Psychiatry
; 25(11): 2786-2799, 2020 11.
Artigo
em Inglês
| MEDLINE | ID: mdl-30116027
4.
Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.
Bioorg Med Chem Lett
; 47: 128193, 2021 09 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-34118412
5.
Discovery of structurally distinct tricyclic M4 positive allosteric modulator (PAM) chemotypes - Part 2.
Bioorg Med Chem Lett
; 53: 128416, 2021 12 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-34710625
6.
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
em Inglês
| MEDLINE | ID: mdl-31248774
7.
Differential Pharmacology and Binding of mGlu2 Receptor Allosteric Modulators.
Mol Pharmacol
; 93(5): 526-540, 2018 05.
Artigo
em Inglês
| MEDLINE | ID: mdl-29545267
8.
The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.
Bioorg Med Chem Lett
; 28(12): 2175-2179, 2018 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29754948
9.
Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype.
Bioorg Med Chem Lett
; 27(11): 2479-2483, 2017 06 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28427812
10.
Discovery of a novel, CNS penetrant M4 PAM chemotype based on a 6-fluoro-4-(piperidin-1-yl)quinoline-3-carbonitrile core.
Bioorg Med Chem Lett
; 27(18): 4274-4279, 2017 09 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-28866269
11.
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M4 positive allosteric modulator (PAM) chemotype via scaffold hopping.
Bioorg Med Chem Lett
; 27(22): 4999-5001, 2017 11 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29037946
12.
Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists.
Bioorg Med Chem Lett
; 27(15): 3576-3581, 2017 08 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28633897
13.
Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides.
Bioorg Med Chem Lett
; 27(13): 2990-2995, 2017 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28522253
14.
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
em Inglês
| MEDLINE | ID: mdl-29089231
15.
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
em Inglês
| MEDLINE | ID: mdl-27939174
16.
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
em Inglês
| MEDLINE | ID: mdl-28442253
17.
Re-exploration of the mGlu1 PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.
Bioorg Med Chem Lett
; 26(9): 2289-92, 2016 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27013388
18.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 3. Engineering plasma stability by discovery and optimization of isoindolinone analogs.
Bioorg Med Chem Lett
; 26(8): 1869-72, 2016 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26988302
19.
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.
Bioorg Med Chem Lett
; 26(3): 751-756, 2016 Feb 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26778256
20.
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.
Bioorg Med Chem Lett
; 25(22): 5107-10, 2015 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26476971