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Jacqueline Agans-Fantuzzi

Explore the profile of Jacqueline Agans-Fantuzzi including associated specialties, affiliations and a list of published articles. Areas
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Articles 8
Citations 123
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Recent Articles
1.
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...
2.
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...
3.
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...
4.
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...
5.
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...
6.
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...
7.
Clasby M, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee W, et al.
Bioorg Med Chem Lett . 2005 Dec; 16(6):1544-8. PMID: 16380251
The design, synthesis, and SAR studies of a structurally novel series of highly potent thrombin receptor (PAR-1) antagonists are described. Compound 30 is a highly potent thrombin receptor antagonist (IC(50)=6.3...
8.
Chackalamannil S, Xia Y, Greenlee W, Clasby M, Doller D, Tsai H, et al.
J Med Chem . 2005 Sep; 48(19):5884-7. PMID: 16161991
Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical PAR-1 antagonist 55 showed a Ki of 2.7 nM in...