Abstract |
Structural variation of the quinolizidine heterocycle of the influenza fusion inhibitor BMY-27709 was examined by several topological dissections in order to illuminate the critical features of the ring system. This exercise resulted in the identification of a series of synthetically more accessible decahydroquinolines that retained the structural elements of BMY-27709 important for antiviral activity. The 2-methyl-cis-decahydroquinoline 6f was the most potent influenza inhibitor identified that demonstrated an EC50 of 90 ng/mL in a plaque reduction assay.
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Authors | K D Combrink, H B Gulgeze, K L Yu, B C Pearce, A K Trehan, J Wei, M Deshpande, M Krystal, A Torri, G Luo, C Cianci, S Danetz, L Tiley, N A Meanwell |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 10
Issue 15
Pg. 1649-52
(Aug 07 2000)
ISSN: 0960-894X [Print] England |
PMID | 10937716
(Publication Type: Journal Article)
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Chemical References |
- Antiviral Agents
- BMY 27709
- Quinolizines
- Salicylamides
- salicylamide
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Topics |
- Animals
- Antiviral Agents
(chemistry, pharmacology)
- Cell Line
- Dogs
- Membrane Fusion
(drug effects)
- Orthomyxoviridae
(drug effects, physiology)
- Quinolizines
(chemistry, pharmacology)
- Salicylamides
(chemistry, pharmacology)
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