Detalhe da pesquisa
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.
Artigo
Inglês
| 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.
Artigo
Inglês
| 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.
Artigo
Inglês
| 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.
Artigo
Inglês
| 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.
Artigo
Inglês
| MEDLINE | ID: mdl-28442253
6.
Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo.
J Neurosci
; 35(21): 8291-6, 2015 May 27.
Artigo
Inglês
| MEDLINE | ID: mdl-26019342
7.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-27476142
8.
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
9.
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
10.
Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.
J Biol Chem
; 285(22): 17054-64, 2010 May 28.
Artigo
Inglês
| MEDLINE | ID: mdl-20356837
11.
Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.
J Biol Chem
; 284(52): 36367-36376, 2009 Dec 25.
Artigo
Inglês
| MEDLINE | ID: mdl-19846549
12.
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Bioorg Med Chem Lett
; 18(1): 49-53, 2008 Jan 01.
Artigo
Inglês
| MEDLINE | ID: mdl-18054229
13.
Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154.
Neuropharmacology
; 128: 492-502, 2018 Jan.
Artigo
Inglês
| MEDLINE | ID: mdl-28729220
14.
Toward ß-Secretase-1 Inhibitors with Improved Isoform Selectivity.
J Med Chem
; 61(8): 3491-3502, 2018 04 26.
Artigo
Inglês
| MEDLINE | ID: mdl-29617572
15.
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.
Artigo
Inglês
| MEDLINE | ID: mdl-28197318
16.
Tumor cell sensitization to apoptotic stimuli by selective inhibition of specific Akt/PKB family members.
Mol Cancer Ther
; 4(2): 271-9, 2005 Feb.
Artigo
Inglês
| MEDLINE | ID: mdl-15713898
17.
Identification of a Chrysanthemic Ester as an Apolipoprotein E Inducer in Astrocytes.
PLoS One
; 11(9): e0162384, 2016.
Artigo
Inglês
| MEDLINE | ID: mdl-27598782
18.
State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects.
Neuropharmacology
; 102: 244-53, 2016 Mar.
Artigo
Inglês
| MEDLINE | ID: mdl-26617071
19.
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
J Med Chem
; 45(26): 5640-8, 2002 Dec 19.
Artigo
Inglês
| MEDLINE | ID: mdl-12477347
20.
Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.
J Med Chem
; 47(24): 5825-8, 2004 Nov 18.
Artigo
Inglês
| MEDLINE | ID: mdl-15537338