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Synthesis of a small library of non-symmetric cyclic sulfamide HIV-1 protease inhibitors
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
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2010 (English)In: Tetrahedron, ISSN 0040-4020, E-ISSN 1464-5416, Vol. 66, no 23, 4049-4056 p.Article in journal (Refereed) Published
Abstract [en]

A set of 11 non-symmetric cyclic sulfamide HIV-1 protease inhibitors were synthesized and evaluated. The use of a key microwave-assisted silver(I) oxide mediated selective mono N-benzylation reaction enabled fast and straightforward synthesis. The K-i values of the new inhibitors ranged between 0.28 mu M and >20 mu M.

Place, publisher, year, edition, pages
2010. Vol. 66, no 23, 4049-4056 p.
Keyword [en]
HIV-1, Protease inhibitor, Microwave, Palladium catalysis, Benzylation
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-136062DOI: 10.1016/j.tet.2010.04.023ISI: 000278198000011OAI: oai:DiVA.org:uu-136062DiVA: diva2:376130
Available from: 2010-12-10 Created: 2010-12-09 Last updated: 2017-12-11Bibliographically approved

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Hallberg, AndersKarlén, AndersLarhed, Mats

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