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1.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-31248774
2.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-28522253
3.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-29089231
4.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-27939174
5.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-28442253
6.
Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition.
Bioorg Med Chem Lett
; 26(17): 4282-6, 2016 09 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-27476142
7.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-27185330
8.
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Bioorg Med Chem Lett
; 23(10): 2996-3000, 2013 May 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-23562060
9.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-23177787
10.
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.
Artículo
en Inglés
| MEDLINE | ID: mdl-30076050
11.
Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.
Bioorg Med Chem Lett
; 22(15): 5084-8, 2012 Aug 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-22738637
12.
Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia.
ACS Med Chem Lett
; 8(2): 233-238, 2017 Feb 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-28197318
13.
Application of Parallel Multiparametric Cell-Based FLIPR Detection Assays for the Identification of Modulators of the Muscarinic Acetylcholine Receptor 4 (M4).
J Biomol Screen
; 20(7): 858-68, 2015 Aug.
Artículo
en Inglés
| MEDLINE | ID: mdl-25877150
14.
Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).
J Med Chem
; 57(18): 7804-10, 2014 Sep 25.
Artículo
en Inglés
| MEDLINE | ID: mdl-25147929
15.
Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
ACS Chem Neurosci
; 5(10): 920-42, 2014 Oct 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-25137629
16.
Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.
ACS Chem Neurosci
; 3(12): 1025-36, 2012 Dec 19.
Artículo
en Inglés
| MEDLINE | ID: mdl-23259038
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