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Microwave-accelerat...
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold
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- Ekegren, Jenny K (author)
- Uppsala universitet,Institutionen för läkemedelskemi
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- Ginman, Nina (author)
- Uppsala universitet,Institutionen för cell- och molekylärbiologi
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- Johansson, Åsa (author)
- Uppsala universitet,Institutionen för läkemedelskemi
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Wallberg, Hans (author)
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- Larhed, Mats (author)
- Uppsala universitet,Institutionen för läkemedelskemi
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Samuelsson, Bertil (author)
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- Unge, Torsten (author)
- Uppsala universitet,Institutionen för cell- och molekylärbiologi
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- Hallberg, Anders (author)
- Uppsala universitet,Institutionen för läkemedelskemi
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(creator_code:org_t)
- 2006-02-11
- 2006
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 49:5, s. 1828-1832
- Related links:
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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- 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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Farmaceutiska vetenskaper (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Pharmaceutical Sciences (hsv//eng)
Keyword
- PHARMACY
- FARMACI
Publication and Content Type
- ref (subject category)
- art (subject category)
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