John Clader
Overview
Explore the profile of John Clader including associated specialties, affiliations and a list of published articles.
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Articles
15
Citations
66
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Recent Articles
1.
Wu W, Burnett D, Clader J, Greenlee W, Jiang Q, Hyde L, et al.
Bioorg Med Chem Lett
. 2016 Nov;
26(23):5836-5841.
PMID: 27836402
In this paper we describe our strategy to improve the aqueous solubility of SCH 900229, a potent PS1-selective γ-secretase inhibitor for the treatment of Alzheimer's disease. Incorporation of ionizable amino...
2.
McKittrick B, Caldwell J, Bara T, Boykow G, Chintala M, Clader J, et al.
Bioorg Med Chem Lett
. 2015 Mar;
25(7):1592-6.
PMID: 25728416
The development of renin inhibitors with favorable oral pharmacokinetic profiles has been a longstanding challenge for the pharmaceutical industry. As part of our work to identify inhibitors of BACE1, we...
3.
Huang X, Zhou W, Liu X, Li H, Sun G, Mandal M, et al.
ACS Med Chem Lett
. 2014 Jun;
3(11):931-5.
PMID: 24900409
Fused oxadiazines (3) were discovered as selective and orally bioavailable γ-secretase modulators (GSMs) based on the structural framework of oxadiazoline GSMs. Although structurally related, initial modifications showed that structure-activity relationships...
4.
Wu W, Domalski M, Burnett D, Josien H, Bara T, Rajagopalan M, et al.
ACS Med Chem Lett
. 2014 Jun;
3(11):892-6.
PMID: 24900404
An exploration of the SAR of the side chain of a novel tricyclic series of γ-secretase inhibitors led to the identification of compound (-)-16 (SCH 900229), which is a potent...
5.
Wu W, Sasikumar T, Domalski M, Qiang L, Burnett D, Clader J, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(3):850-3.
PMID: 23265902
Attempts to block metabolism by incorporating a 9-fluoro substituent at the A-ring of compound 1 (SCH 900229) using electrophilic Selectfluor™ led to an unexpected oxidation of the A-ring to give...
6.
Wu W, Asberom T, Bara T, Bennett C, Burnett D, Clader J, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(3):844-9.
PMID: 23265892
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective γ-secretase inhibitor and clinical candidate for the...
7.
Li H, Qin J, Dhondi P, Zhou W, Vicarel M, Bara T, et al.
Bioorg Med Chem Lett
. 2012 Dec;
23(2):466-71.
PMID: 23253441
In an attempt to further improve overall profiles of the oxadiazine series of GSMs, in particular the hERG activity, conformational modifications of the core structure resulted in the identification of...
8.
Sun Z, Asberom T, Bara T, Bennett C, Burnett D, Chu I, et al.
J Med Chem
. 2011 Nov;
55(1):489-502.
PMID: 22098494
Cyclic hydroxyamidines were designed and validated as isosteric replacements of the amide functionality. Compounds with these structural motifs were found to be metabolically stable and to possess highly desirable pharmacokinetic...
9.
Lee J, Song L, Terracina G, Bara T, Josien H, Asberom T, et al.
Biochemistry
. 2011 May;
50(22):4973-80.
PMID: 21528914
Accumulation of the β-amyloid (Aβ) peptides is one of the major pathologic hallmarks in the brains of Alzheimer's disease (AD) patients. Aβ is generated by sequential proteolytic cleavage of the...
10.
Qin J, Dhondi P, Huang X, Mandal M, Zhao Z, Pissarnitski D, et al.
Bioorg Med Chem Lett
. 2011 Jan;
21(2):664-9.
PMID: 21195610
We herein report the discovery of four series of fused 5,6-bicyclic heterocycles as γ-secretase modulators. Synthesis and SAR of these series are discussed. These compounds represent a new class of...