John A Wos
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Explore the profile of John A Wos including associated specialties, affiliations and a list of published articles.
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20
Citations
50
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Recent Articles
1.
Tian X, Switzer A, Derose S, Mishra R, Solinsky M, Mumin R, et al.
J Med Chem
. 2008 Sep;
51(19):6055-66.
PMID: 18771254
A study that was designed to identify plausible replacements for highly basic guanidine moiety contained in potent MC4R agonists, as exemplified by 1, led to the discovery of initial nonguanidine...
2.
Mendez-Andino J, Wos J
Drug Discov Today
. 2007 Nov;
12(21-22):972-9.
PMID: 17993417
Despite the high number of drug-discovery programs dedicated to finding small-molecule MCH-R1 antagonists for the treatment of obesity and/or mood disorders, a very limited number of these have progressed into...
3.
Eric Hu X, Wos J, Dowty M, Suchanek P, Ji W, Chambers J, et al.
J Pharmacol Exp Ther
. 2007 Oct;
324(1):206-13.
PMID: 17932246
The melanin-concentrating hormone-1 receptor (MCH1R) is a G-protein-coupled receptor expressed in the brain and peripheral tissues that regulates energy storage and body weight. Here, we focused on discovery of the...
4.
Mendez-Andino J, Colson A, Meyers K, Mitchell M, Hodge K, Howard J, et al.
Bioorg Med Chem
. 2007 Jan;
15(5):2092-105.
PMID: 17236777
The design, synthesis, and biological studies of a novel class of MCH-R1 antagonists based on an aminotetrahydronaphthalene ketopiperazine scaffold is described. Compounds within this class promoted significant body weight reduction...
5.
Meyers K, Mendez-Andino J, Colson A, Eric Hu X, Wos J, Mitchell M, et al.
Bioorg Med Chem Lett
. 2006 Dec;
17(3):657-61.
PMID: 17174091
The synthesis and biological testing of novel classes of potent melanin-concentrating hormone (MCH-R1) antagonists based on pyrazolopiperazinone and pyrrolopiperazinone scaffolds are described.
6.
Wang Y, ONeil S, Wos J, Oppong K, Laufersweiler M, Soper D, et al.
Bioorg Med Chem
. 2006 Nov;
15(3):1311-22.
PMID: 17127070
Peptidomimetic compounds possessing a caprolactam ring constraint were prepared and evaluated as interleukin-1beta converting enzyme (ICE) inhibitors. The caprolactam ring was used to constrain the P3 region of our inhibitors....
7.
Meyers K, Mendez-Andino J, Colson A, Warshakoon N, Wos J, Mitchell M, et al.
Bioorg Med Chem Lett
. 2006 Nov;
17(3):819-22.
PMID: 17107796
A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were...
8.
Meyers K, Kim N, Mendez-Andino J, Eric Hu X, Mumin R, Klopfenstein S, et al.
Bioorg Med Chem Lett
. 2006 Nov;
17(3):814-8.
PMID: 17107791
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists with greater selectivity over hERG were identified. SAR studies addressing two distinct alternatives for structural modifications leading to improve hERG selectivity are described.
9.
Soper D, Sheville J, ONeil S, Wang Y, Laufersweiler M, Oppong K, et al.
Bioorg Med Chem
. 2006 Aug;
14(23):7880-92.
PMID: 16908171
An 8,5-fused bicyclic peptidomimetic ring system generated by a stereoselective ring metathesis reaction was elaborated into potent inhibitors of interleukin-1beta converting enzyme (ICE, caspase-1). Multiple compounds were found that exhibited...
10.
Kim N, Meyers K, Mendez-Andino J, Warshakoon N, Ji W, Wos J, et al.
Bioorg Med Chem Lett
. 2006 Aug;
16(20):5445-50.
PMID: 16879961
A substituted 4-aminopiperidine was identified as showing activity in an MCH assay from an HTS effort. Subsequent structural modification of the scaffold led to the identification of a number of...