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77953869314
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For synthetic procedures, see: WO 2009042093
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For synthetic procedures, see: Coburn, C. A.; Vacca, J. P.; Rajapakse, H. A.; Jones, K. L. G.; Nantermet, P.; Barrow, J. C.; Moore, K. P.; Sharik, S. S.; Theberge, C.; Walji, A. M. WO 2009042093.
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8944254642
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R = iPr was prepared from 1-iodo-2-methylpropane and catalytic base, tetramethylguanidine, see: 1958, 38, 75
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R = iPr was prepared from 1-iodo-2-methylpropane and catalytic base, tetramethylguanidine, see:. Kornblum N., and Ungnade H.E. Org. Synth. 4 (1963) 724 1958, 38, 75
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77953872919
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note
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2Me, 1 N NaOH, 77%, followed by N-hydroxysuccinimide, DCC, dioxane, 0 °C.
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16
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0028222149
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95) are defined as those which inhibited by 95% the spread of HIV-1 infection in susceptible cell culture. MT-4 human T-lymphoid cells were maintained in RPMI 1640 medium containing 10% heat inactivated fetal bovine serum. Cells were infected en masse at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24 h. At this time, cells were washed and distributed into 96 well microtiter dishes. Cells were resuspended in media containing 50% normal human serum (Lonza). 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 at 4 days
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95) are defined as those which inhibited by 95% the spread of HIV-1 infection in susceptible cell culture. MT-4 human T-lymphoid cells were maintained in RPMI 1640 medium containing 10% heat inactivated fetal bovine serum. Cells were infected en masse at low multiplicity (0.01) using HIV-1 strain IIIb and were incubated for 24 h. At this time, cells were washed and distributed into 96 well microtiter dishes. Cells were resuspended in media containing 50% normal human serum (Lonza). 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 at 4 days
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Vacca, J.P.1
Dorsey, B.D.2
Schleif, W.A.3
Levin, R.B.4
McDaniel, S.L.5
Darke, P.L.6
Zugay, J.7
Quintero, J.C.8
Blahy, O.M.9
Roth, E.10
Sardana, V.V.11
Schlabac, A.J.12
Graham, P.I.13
Condra, J.H.14
Gotlib, L.15
Holloway, M.K.16
Lin, J.17
Chen, I.-W.18
Vastag, K.19
Ostovic, D.20
Anderson, P.S.21
Emini, E.E.22
Huff, J.R.23
more..
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17
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84855622587
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Version 8.5.207, Schrödinger, LLC, New York, NY, www.schrodinger.com.
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Version 8.5.207, Schrödinger, LLC, New York, NY, www.schrodinger.com.
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19
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0034019566
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Phenotypic drug susceptibility assay performed by Monogram Biosciences, see:
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Phenotypic drug susceptibility assay performed by Monogram Biosciences, see:. Petropoulos C.J., Parkin N.T., Limoli K.L., Lie Y.S., Wrin T., Huang W., Tian H., Smith D., Winslow G.A., Capon D.J., and Whitcomb J.M. Antimicrob. Agents Chemother. 44 (2000) 920
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Petropoulos, C.J.1
Parkin, N.T.2
Limoli, K.L.3
Lie, Y.S.4
Wrin, T.5
Huang, W.6
Tian, H.7
Smith, D.8
Winslow, G.A.9
Capon, D.J.10
Whitcomb, J.M.11
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