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7
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17744420893
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Smith H.K., Beckett R.P., Clements J.M., Doel S., East S.P., Launchbury S.B., Pratt L.M., Spavold Z.M., Thomas W., Todd R.S., Whittaker M. Bioorg. Med. Chem. Lett. 12:2002;3595.
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Smith, H.K.1
Beckett, R.P.2
Clements, J.M.3
Doel, S.4
East, S.P.5
Launchbury, S.B.6
Pratt, L.M.7
Spavold, Z.M.8
Thomas, W.9
Todd, R.S.10
Whittaker, M.11
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8
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12444268598
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(a) Davies S.J., Ayscough A.P., Beckett R.P., Bragg R.A., Clements J.M., Doel S., Grew C., Launchbury S.B., Perkins G.M., Pratt L.M., Smith H.K., Spavold Z.M., Thomas S.W., Todd R.S., Whittaker M. Bioorg. Med. Chem. Lett. 13:2003;2709
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Bioorg. Med. Chem. Lett.
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Davies, S.J.1
Ayscough, A.P.2
Beckett, R.P.3
Bragg, R.A.4
Clements, J.M.5
Doel, S.6
Grew, C.7
Launchbury, S.B.8
Perkins, G.M.9
Pratt, L.M.10
Smith, H.K.11
Spavold, Z.M.12
Thomas, S.W.13
Todd, R.S.14
Whittaker, M.15
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9
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0037811323
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(b) Davies S.J., Ayscough A.P., Beckett R.P., Clements J.M., Doel S., Pratt L.M., Spavold Z.M., Thomas S.W., Whittaker M. Bioorg. Med. Chem. Lett. 13:2003;2715.
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Davies, S.J.1
Ayscough, A.P.2
Beckett, R.P.3
Clements, J.M.4
Doel, S.5
Pratt, L.M.6
Spavold, Z.M.7
Thomas, S.W.8
Whittaker, M.9
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10
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85030916476
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note
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The tertiary alcohol, general formula 14, resulting from double addition of the metallated species to Pfp ester 3 was usually detected as a side product (typically ~10%) in this reaction.
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11
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0035829139
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Pratt L.M., Beckett R.P., Davies S.J., Launchbury S.B., Miller A., Spavold Z.M., Todd R.S., Whittaker M. Bioorg. Med. Chem. Lett. 11:2001;2585.
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Pratt, L.M.1
Beckett, R.P.2
Davies, S.J.3
Launchbury, S.B.4
Miller, A.5
Spavold, Z.M.6
Todd, R.S.7
Whittaker, M.8
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12
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85030933689
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note
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Full experimental details on individual compounds can be found in the patent literature. International publication number: WO 00/61134.
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13
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85030933939
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note
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The natural ferrous-containing PDF enzyme oxidises readily to the inactive ferric form. Consequently, for ease of experimentation, we routinely test against the stable nickel-containing enzyme that retains full catalytic activity.
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14
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0035143273
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For details of the PDF inhibition and microbiological assays see: Clements J.M., Beckett R.P., Brown A., Catlin G., Lobell M., Palan S., Thomas W., Whittaker M., Wood S., Salama S., Baker P.J., Rodgers H.F., Barynin V., Rice D.W., Hunter M.G. Antimicrob. Agents Chemother. 45:2001;563.
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, vol.45
, pp. 563
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Clements, J.M.1
Beckett, R.P.2
Brown, A.3
Catlin, G.4
Lobell, M.5
Palan, S.6
Thomas, W.7
Whittaker, M.8
Wood, S.9
Salama, S.10
Baker, P.J.11
Rodgers, H.F.12
Barynin, V.13
Rice, D.W.14
Hunter, M.G.15
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16
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0346549896
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Koga H., Itoh A., Murayama S., Suzue S., Irikura T. J. Med. Chem. 23:1980;1258.
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J. Med. Chem.
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, pp. 1258
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Koga, H.1
Itoh, A.2
Murayama, S.3
Suzue, S.4
Irikura, T.5
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17
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85030917035
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note
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19F NMR experiments. Only the 2-aminoaryl ketones were isolated following purification.
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18
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0034878770
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Margolis P., Hackbath C., Lopez S., Maniar M., Wang W., Yuan Z., White R., Trias J. Antimicrob. Agents Chemother. 45:2001;2432.
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(2001)
Antimicrob. Agents Chemother.
, vol.45
, pp. 2432
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Margolis, P.1
Hackbath, C.2
Lopez, S.3
Maniar, M.4
Wang, W.5
Yuan, Z.6
White, R.7
Trias, J.8
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19
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85030931934
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note
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All compounds were tested against an fmt mutant strain of S. aureus and shown to have an MIC gt;32 μg/mL. From this result we infer that PDF inhibition is the mechanism of action.
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