Ho-Sam Ahn
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Explore the profile of Ho-Sam Ahn including associated specialties, affiliations and a list of published articles.
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Articles
14
Citations
150
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Recent Articles
1.
Chelliah M, Eagen K, Guo Z, Chackalamannil S, Xia Y, Tsai H, et al.
ACS Med Chem Lett
. 2014 Jun;
5(5):561-5.
PMID: 24900880
We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar....
2.
Chelliah M, Chackalamannil S, Xia Y, Greenlee W, Ahn H, Kurowski S, et al.
ACS Med Chem Lett
. 2014 Jun;
5(2):183-7.
PMID: 24900795
We have synthesized several C7-aminomethyl analogues of vorapaxar that are potent PAR-1 antagonists. Many of these analogues showed excellent in vitro binding affinity and pharmacokinetics profile in rats. Compound 6a...
3.
Chelliah M, Chackalamannil S, Xia Y, Eagen K, Greenlee W, Ahn H, et al.
Bioorg Med Chem Lett
. 2012 Mar;
22(7):2544-9.
PMID: 22405832
Discovery of a novel nor-seco himbacine analog as potent thrombin receptor (PAR-1) antagonist is described. Despite low plasma level, these new analogs showed excellent ex vivo efficacy in the monkey...
4.
Xia Y, Chackalamannil S, Greenlee W, Wang Y, Hu Z, Root Y, et al.
Bioorg Med Chem Lett
. 2010 Oct;
20(22):6676-9.
PMID: 20888225
An analog of the thrombin receptor antagonist vorapaxar (SCH 530348) with increased aqueous solubility, compound 9c (SCH 602539), was discovered through incorporation of polar substituents on the pyridine ring of...
5.
Chackalamannil S, Wang Y, Greenlee W, Hu Z, Xia Y, Ahn H, et al.
J Med Chem
. 2008 May;
51(11):3061-4.
PMID: 18447380
The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of this series has led to the discovery of...
6.
Chelliah M, Chackalamannil S, Xia Y, Eagen K, Clasby M, Gao X, et al.
J Med Chem
. 2007 Sep;
50(21):5147-60.
PMID: 17854166
Pursuing our earlier efforts in the himbacine-based thrombin receptor antagonist area, we have synthesized a series of compounds that incorporate heteroatoms in the C-ring of the tricyclic motif. This effort...
7.
Xia Y, Chackalamannil S, Clasby M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2007 Jun;
17(16):4509-13.
PMID: 17574850
The structure-activity relationship (SAR) of the vinyl pyridine region of himbacine derived thrombin receptor (PAR-1) antagonists is described. A 2-vinylpyridyl ring substituted with an aryl or a heteroaryl group at...
8.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett
. 2007 May;
17(13):3647-51.
PMID: 17490877
The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and in vivo potency. The most potent...
9.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
J Med Chem
. 2007 Jan;
50(1):129-38.
PMID: 17201416
The metabolism of our prototypical thrombin receptor antagonist 1, Ki = 2.7 nM, was studied and three major metabolites (2, 4, and 5) were found. The structures of the metabolites...
10.
Xia Y, Chackalamannil S, Chan T, Czarniecki M, Doller D, Eagen K, et al.
Bioorg Med Chem Lett
. 2006 Jul;
16(18):4969-72.
PMID: 16824760
The structure-activity relationship (SAR) of the lactone ring of himbacine derived thrombin receptor (PAR-1) antagonists (e.g., 2-5) is described. The effect of the lactone carbonyl group on binding to PAR-1...