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95) is defined as the concentration of agent that inhibits the spread of HIV-1 infection in susceptible cell culture by 95%. MT4 human T-lymphoid cells were maintained in RPMI-1640 medium containing 10% heat-inactivated fetal bovine serum. Cells were infected all together at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24h. At this time, cells were washed and distributed into 96-well microtiter dishes. Serial twofold dilutions of inhibitor were added to the wells, and the cultures were maintained for three additional days. Virus spread was assessed by HIV-1 P24 core antigen ELISA. Control cultures in the absence of inhibitor were fully infected after four days.
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95) is defined as the concentration of agent that inhibits the spread of HIV-1 infection in susceptible cell culture by 95%. MT4 human T-lymphoid cells were maintained in RPMI-1640 medium containing 10% heat-inactivated fetal bovine serum. Cells were infected all together at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24h. At this time, cells were washed and distributed into 96-well microtiter dishes. Serial twofold dilutions of inhibitor were added to the wells, and the cultures were maintained for three additional days. Virus spread was assessed by HIV-1 P24 core antigen ELISA. Control cultures in the absence of inhibitor were fully infected after four days.
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For the discovery of benzyl alcohols see the following patent: J. W. Erickson, S. V. Gulnik, A. K. Ghosh, K. A. Hussain, (National Institutes of Health; Rockville, USA; University of Illinois, Urbana, USA), WO/1999/067254, 1999.
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2) via chelation-controlled organo Grignard addition; for details see, -
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3 via an open transition state, the (R)-isomer of the chiral auxiliary was used; for details see: G. K. Prakash, M. Mandal, J. Am. Chem. Soc. 2002, 124, 6538-6539.
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A fluorescence resonance energy transfer (FRET)-based assay using HIV protease substrate Ser-Gln-Asn-(β-naphthylalanine)-Pro-Ile-Val.
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A fluorescence resonance energy transfer (FRET)-based assay using HIV protease substrate Ser-Gln-Asn-(β-naphthylalanine)-Pro-Ile-Val.
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79251540378
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The diastereomers were separable by silica gel chromatography at stepj in Scheme2 or by preparative HPLC at stepl in Scheme2.
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The diastereomers were separable by silica gel chromatography at stepj in Scheme2 or by preparative HPLC at stepl in Scheme2.
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For comparison, the in vitro potency of darunavir (DRV) in our 10% and 50% serum-shifted SPREAD assays are 9 and 23nm, respectively.
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For comparison, the in vitro potency of darunavir (DRV) in our 10% and 50% serum-shifted SPREAD assays are 9 and 23nm, respectively.
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