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5. Syntheses of R,Snaproxen and its 6Odesmethylated metabolite labelled with 2H

Author

Fontana, E. and Venegoni, S.

Abstract

Naproxen, a wellknown nonsteroidal antiinflammatory drug, and its 6Odesmethylated metabolite have been labelled with 2H. R,SNaproxen 7 labelled with 2H was obtained in five steps using the commercially available 2H3iodomethane 5 as the stable labelled reagent. The demethylation of 7 using 48 HBr in 1butyl3methylimidazolium tetrafluoborate gave the corresponding 2Hlabelled 6Odesmethylated metabolite 8. Copyright © 2008 John Wiley & Sons, Ltd.

Published
2008
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6. Design, synthesis, and biological evaluation of new (2E,6E)-10-(dimethylamino)-3,7-dimethyl-2,6-decadien-1-ol ethers as inhibitors of human and Trypanosoma cruzi oxidosqualene cyclase.

Author

Galli U, Oliaro-Bosso S, Taramino S, Venegoni S, Pastore E, Tron GC, Balliano G, Viola F, and Sorba G

Subjects
Animals, Antiparasitic Agents chemical synthesis, Drug Design, Enzyme Inhibitors chemical synthesis, Humans, Phenyl Ethers chemical synthesis, Phenyl Ethers chemistry, Phenyl Ethers pharmacology, Antiparasitic Agents chemistry, Antiparasitic Agents pharmacology, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacology, Intramolecular Transferases antagonists & inhibitors, Squalene analogs & derivatives, Trypanosoma cruzi enzymology
Abstract

New dimethylamino truncated squalene ether derivatives containing a different aromatic moiety (phenyl, naphthyl, and biphenyl) or a simple alkyl (n-hexylic) group were synthesized as inhibitors of the oxidosqualene cyclase (OSC) and of the sterol biosynthetic pathway. The activity against human OSC was compared with the activity against the OSCs of pathogenic organisms such as Pneumocystis carinii and Trypanosoma cruzi. The phenyl derivative was the most potent inhibitor of T. cruzi OSC.

Published
2007
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7. Against all odds.

Author

Modigh A and Venegoni SL

Subjects
Geriatric Nursing standards, Health Facility Closure, Humans, Missouri, Administrative Personnel, Nurse Administrators, Nurse Practitioners, Nursing Homes organization & administration, Quality Assurance, Health Care organization & administration
Published
1988
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