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Design and Synthesis of P1-P3 Macrocyclic Tertiary-Alcohol-Comprising HIV-1 Protease Inhibitors
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
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2013 (English)In: Journal of Medicinal Chemistry, ISSN 0022-2623, E-ISSN 1520-4804, Vol. 56, no 22, 8999-9007 p.Article in journal (Refereed) Published
Abstract [en]

To study P1-P3 macrocyclizations of previously reported tertiary-alcohol-comprising HIV-1 protease inhibitors (PIs), three new 14- and 15-member macrocyclic PIs were designed, synthesized by ring-closing metathesis, and evaluated alongside with 10 novel linear PIs. Cocrystallized complexes of the macrocyclic PIs and the HIV-1 protease are presented, analyzed, and discussed. The macrocyclic structures exhibited higher activities than the linear precursors with K-i and EC50 values down to 3.1 nM and 0.37 mu M, respectively.

Place, publisher, year, edition, pages
2013. Vol. 56, no 22, 8999-9007 p.
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Medical and Health Sciences
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URN: urn:nbn:se:uu:diva-214038DOI: 10.1021/jm400811dISI: 000327812600004OAI: oai:DiVA.org:uu-214038DiVA: diva2:684180
Available from: 2014-01-07 Created: 2014-01-07 Last updated: 2017-12-06Bibliographically approved

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Hallberg, AndersLarhed, Mats

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