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Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
Uppsala University, Disciplinary Domain of Science and Technology, Biology, Department of Cell and Molecular Biology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry.
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2006 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 49, no 5, 1828-1832 p.Article in journal (Refereed) Published
Abstract [en]

Two series of P1'-extended HIV-1 protease inhibitors comprising a tertiary alcohol in the transition-state mimic exhibiting Ki values ranging from 2.1 to 93 nM have been synthesized. Microwave-accelerated palladium-catalyzed cross-couplings were utilized to rapidly optimize the P1' side chain. High cellular antiviral potencies were encountered when the P1' benzyl group was elongated with a 3- or 4-pyridyl substituent (EC50 = 0.18-0.22 microM). X-ray crystallographic data were obtained for three inhibitors cocrystallized with the enzyme.

Place, publisher, year, edition, pages
2006. Vol. 49, no 5, 1828-1832 p.
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Pharmaceutical Sciences
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URN: urn:nbn:se:uu:diva-24527DOI: 10.1021/jm051239zISI: 000236005400033PubMedID: 16509598OAI: oai:DiVA.org:uu-24527DiVA: diva2:52301
Available from: 2008-01-29 Created: 2008-01-29 Last updated: 2017-12-07Bibliographically approved

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Larhed, MatsUnge, TorstenHallberg, Anders

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