(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor
Publication
, Journal Article
Kirkup, MP; Rizvi, R; Shankar, BB; Dugar, S; Clader, JW; McCombie, SW; Lin, SI; Yumibe, N; Huie, K; Van Heek, M; Compton, DS; Davis, HR; McPhail, AT
Published in: Bioorganic and Medicinal Chemistry Letters
September 3, 1996
Previous SAR studies of C-3 side chain modified analogs of (-)-SCH 48461, as well as information concerning the metabolic stability this series, enabled us to design a cholesterol absorption inhibitor (i.e., (-) 2a, SCH 57939) with tenfold higher potency and greatly enhanced metabolic stability. The synthesis and pharmacological profile, including the role of relative stereochemistry at both the C3 and 1' positions in determining the SAR of these compounds, will be discussed.
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Published In
Bioorganic and Medicinal Chemistry Letters
DOI
ISSN
0960-894X
Publication Date
September 3, 1996
Volume
6
Issue
17
Start / End Page
2069 / 2072
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry
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Kirkup, M. P., Rizvi, R., Shankar, B. B., Dugar, S., Clader, J. W., McCombie, S. W., … McPhail, A. T. (1996). (-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor. Bioorganic and Medicinal Chemistry Letters, 6(17), 2069–2072. https://doi.org/10.1016/0960-894X(96)00365-4
Kirkup, M. P., R. Rizvi, B. B. Shankar, S. Dugar, J. W. Clader, S. W. McCombie, S. I. Lin, et al. “(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor.” Bioorganic and Medicinal Chemistry Letters 6, no. 17 (September 3, 1996): 2069–72. https://doi.org/10.1016/0960-894X(96)00365-4.
Kirkup MP, Rizvi R, Shankar BB, Dugar S, Clader JW, McCombie SW, et al. (-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor. Bioorganic and Medicinal Chemistry Letters. 1996 Sep 3;6(17):2069–72.
Kirkup, M. P., et al. “(-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor.” Bioorganic and Medicinal Chemistry Letters, vol. 6, no. 17, Sept. 1996, pp. 2069–72. Scopus, doi:10.1016/0960-894X(96)00365-4.
Kirkup MP, Rizvi R, Shankar BB, Dugar S, Clader JW, McCombie SW, Lin SI, Yumibe N, Huie K, Van Heek M, Compton DS, Davis HR, McPhail AT. (-)-SCH 57939: Synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor. Bioorganic and Medicinal Chemistry Letters. 1996 Sep 3;6(17):2069–2072.
Published In
Bioorganic and Medicinal Chemistry Letters
DOI
ISSN
0960-894X
Publication Date
September 3, 1996
Volume
6
Issue
17
Start / End Page
2069 / 2072
Related Subject Headings
- Medicinal & Biomolecular Chemistry
- 3405 Organic chemistry
- 3404 Medicinal and biomolecular chemistry
- 1115 Pharmacology and Pharmaceutical Sciences
- 0305 Organic Chemistry
- 0304 Medicinal and Biomolecular Chemistry