2cej: Difference between revisions
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==Overview== | ==Overview== | ||
Two series of P1'-extended HIV-1 protease inhibitors comprising a tertiary | 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. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Human immunodeficiency virus 1]] | [[Category: Human immunodeficiency virus 1]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Ekegren, J | [[Category: Ekegren, J K.]] | ||
[[Category: Ginman, N.]] | [[Category: Ginman, N.]] | ||
[[Category: Hallberg, A.]] | [[Category: Hallberg, A.]] | ||
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[[Category: protease]] | [[Category: protease]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:47:47 2008'' | ||