-
2
-
-
0035927426
-
-
(a) For recent reviews, see: Wolfe M.S. J. Med. Chem. 44:2001;2039
-
(2001)
J. Med. Chem.
, vol.44
, pp. 2039
-
-
Wolfe, M.S.1
-
6
-
-
0025295039
-
-
Esch F.S., Keim P.S., Beattie E.C., Blacher R.W., Culwell A.R., Oltersdorf T., McClure D., Ward P.J. Science. 248:1990;1122.
-
(1990)
Science
, vol.248
, pp. 1122
-
-
Esch, F.S.1
Keim, P.S.2
Beattie, E.C.3
Blacher, R.W.4
Culwell, A.R.5
Oltersdorf, T.6
McClure, D.7
Ward, P.J.8
-
7
-
-
0033946796
-
-
Rishton G.M., Retz D.M., Tempest P.A., Novotny J., Kahn S., Treanor J.J.S., Lile J.D., Citron M. J. Med. Chem. 43:2000;2297.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 2297
-
-
Rishton, G.M.1
Retz, D.M.2
Tempest, P.A.3
Novotny, J.4
Kahn, S.5
Treanor, J.J.S.6
Lile, J.D.7
Citron, M.8
-
8
-
-
0034618705
-
-
Moore C.L., Leatherwood D.D., Diehl T.S., Selkoe D.J., Wolfe M.S. J. Med. Chem. 43:2000;3434.
-
(2000)
J. Med. Chem.
, vol.43
, pp. 3434
-
-
Moore, C.L.1
Leatherwood, D.D.2
Diehl, T.S.3
Selkoe, D.J.4
Wolfe, M.S.5
-
9
-
-
0035163347
-
-
Dovey H.F., John V., Anderson J.P., Chen L.Z., de Saint Andrieu P., Fang L.Y., Freedman S.B., Folmer B., Goldbach E., Holsztynska E.J., Hu K.L., Johnson-Wood K.L., Kennedy S.L., Kholodenko D., Knops J.E., Latimer L.H., Lee M., Liao Z., Lieberburg I.M., Motter R.N., Mutter L.C., Nietz J., Quinn K.P., Sacchi K.L., Seubert P.A., Shopp G.M., Thorsett E.D., Tung J.S., Wu J., Yang S., Yin C.T., Schenk D.B., May P.C., Altstiel L.D., Bender M.H., Boggs L.N., Britton T.C., Clemens J.C., Czilli D.L., Dieckman-McGinty D.K., Droste J.J., Fuson K.S., Gitter B.D., Hyslop P.A., Johnstone E.M., Li W.-Y., Little S.P., Mabry T.E., Miller F.D., Ni B., Nissen J.S., Porter W.J., Potts B.D., Reel J.K., Stephenson D., Su Y., Shipley L.A., Whitesitt C.A., Yin T., Audia J.E. J. Neurochem. 76:2001;173.
-
(2001)
J. Neurochem.
, vol.76
, pp. 173
-
-
Dovey, H.F.1
John, V.2
Anderson, J.P.3
Chen, L.Z.4
De Saint Andrieu, P.5
Fang, L.Y.6
Freedman, S.B.7
Folmer, B.8
Goldbach, E.9
Holsztynska, E.J.10
Hu, K.L.11
Johnson-Wood, K.L.12
Kennedy, S.L.13
Kholodenko, D.14
Knops, J.E.15
Latimer, L.H.16
Lee, M.17
Liao, Z.18
Lieberburg, I.M.19
Motter, R.N.20
Mutter, L.C.21
Nietz, J.22
Quinn, K.P.23
Sacchi, K.L.24
Seubert, P.A.25
Shopp, G.M.26
Thorsett, E.D.27
Tung, J.S.28
Wu, J.29
Yang, S.30
Yin, C.T.31
Schenk, D.B.32
May, P.C.33
Altstiel, L.D.34
Bender, M.H.35
Boggs, L.N.36
Britton, T.C.37
Clemens, J.C.38
Czilli, D.L.39
Dieckman-McGinty, D.K.40
Droste, J.J.41
Fuson, K.S.42
Gitter, B.D.43
Hyslop, P.A.44
Johnstone, E.M.45
Li, W.-Y.46
Little, S.P.47
Mabry, T.E.48
Miller, F.D.49
Ni, B.50
Nissen, J.S.51
Porter, W.J.52
Potts, B.D.53
Reel, J.K.54
Stephenson, D.55
Su, Y.56
Shipley, L.A.57
Whitesitt, C.A.58
Yin, T.59
Audia, J.E.60
more..
-
10
-
-
0034254585
-
-
Shearman M.S., Beher D., Clarke E.E., Huw D.L., Harrison T., Hunt P., Nadin A., Smith A.L., Stevenson G., Castro J.L. Biochemistry. 39:2000;8698.
-
(2000)
Biochemistry
, vol.39
, pp. 8698
-
-
Shearman, M.S.1
Beher, D.2
Clarke, E.E.3
Huw, D.L.4
Harrison, T.5
Hunt, P.6
Nadin, A.7
Smith, A.L.8
Stevenson, G.9
Castro, J.L.10
-
12
-
-
85031206351
-
-
WO 0050391
-
Transfected H4 (human neuroglioma) cells stably expressing APP constructs were used to evaluate compounds. The Aβ produced was detected by an ELISA. See: Smith, D. W.; Munoz, B.; Srinirvasan, K.; Bergstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. WO 0050391. See also: Seubert, P.; Vigo-Pelfrey, C.; Esch F.; Lee, M.; Dovey, H.; Davis, D.; Sinha, S.; Schlossmacher, M.; Whaley, J.; Swindlehurst, C.; McCormack, R.; Wolfert, R.; Selkoe, D.; Lieberburg, I.; Schenk, D. Nature 1992, 359, 325.
-
-
-
Smith, D.W.1
Munoz, B.2
Srinirvasan, K.3
Bergstrom, C.P.4
Chaturvedula, P.V.5
Deshpande, M.S.6
Keavy, D.J.7
Lau, W.Y.8
Parker, M.F.9
Sloan, C.P.10
Wallace, O.B.11
Wang, H.H.12
-
13
-
-
0026646605
-
-
Transfected H4 (human neuroglioma) cells stably expressing APP constructs were used to evaluate compounds. The Aβ produced was detected by an ELISA. See: Smith, D. W.; Munoz, B.; Srinirvasan, K.; Bergstrom, C. P.; Chaturvedula, P. V.; Deshpande, M. S.; Keavy, D. J.; Lau, W. Y.; Parker, M. F.; Sloan, C. P.; Wallace, O. B.; Wang, H. H. WO 0050391. See also: Seubert, P.; Vigo-Pelfrey, C.; Esch F.; Lee, M.; Dovey, H.; Davis, D.; Sinha, S.; Schlossmacher, M.; Whaley, J.; Swindlehurst, C.; McCormack, R.; Wolfert, R.; Selkoe, D.; Lieberburg, I.; Schenk, D. Nature 1992, 359, 325.
-
(1992)
Nature
, vol.359
, pp. 325
-
-
Seubert, P.1
Vigo-Pelfrey, C.2
Esch, F.3
Lee, M.4
Dovey, H.5
Davis, D.6
Sinha, S.7
Schlossmacher, M.8
Whaley, J.9
Swindlehurst, C.10
McCormack, R.11
Wolfert, R.12
Selkoe, D.13
Lieberburg, I.14
Schenk, D.15
-
14
-
-
0033598365
-
-
Higaki J.N., Chakravarty S., Bryant C.M., Cowart L.R., Harden P., Scardina J.M., Mavunkel B., Luedtke G.R., Cordell B. J. Med. Chem. 42:1999;3889.
-
(1999)
J. Med. Chem.
, vol.42
, pp. 3889
-
-
Higaki, J.N.1
Chakravarty, S.2
Bryant, C.M.3
Cowart, L.R.4
Harden, P.5
Scardina, J.M.6
Mavunkel, B.7
Luedtke, G.R.8
Cordell, B.9
-
15
-
-
85031198875
-
-
US-05703129, 1997
-
(a) Felsenstein, K.; Smith, D. W.; Poss, M. A.; Chaturvedula, P.; Sloan, C. P. US-05703129, 1997.
-
-
-
Felsenstein, K.1
Smith, D.W.2
Poss, M.A.3
Chaturvedula, P.4
Sloan, C.P.5
-
16
-
-
0033575224
-
-
(b) Durkin J.T., Murthy S., Husten E.J., Trusko S.P., Savage M.J., Rotella D.P., Greenberg B.D., Siman R. J. Biol. Chem. 274:1999;20499
-
(1999)
J. Biol. Chem.
, vol.274
, pp. 20499
-
-
Durkin, J.T.1
Murthy, S.2
Husten, E.J.3
Trusko, S.P.4
Savage, M.J.5
Rotella, D.P.6
Greenberg, B.D.7
Siman, R.8
-
17
-
-
85031205903
-
-
See also ref 7
-
(c) See also ref 7.
-
-
-
-
18
-
-
0001115891
-
-
(a) Matsuda F., Matsumoto T., Ohsaki M., Ito Y., Terashima S. Bull. Chem. Soc. Jpn. 65:1992;360
-
(1992)
Bull. Chem. Soc. Jpn.
, vol.65
, pp. 360
-
-
Matsuda, F.1
Matsumoto, T.2
Ohsaki, M.3
Ito, Y.4
Terashima, S.5
-
22
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85031195249
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note
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The 24 carboxylic acids used were: 1-phenyl-1-cyclopropanecarboxylic acid; 2,2-dichloro-1-methyl-cyclopropanecarboxylic acid; 2,4,5-trimethoxy-alpha-methylcinnamic acid; 2-oxo-6-pentyl-2H-pyran-3-carboxylic acid; 3-(3-methoxyphenyl)propionic acid; 3-(phenylsulfonyl)propionic acid; 3,4-(methylenedioxy)-phenylacetic acid; 3,5-bis(trifluoromethyl)phenylacetic acid; 3,5-difluorophenylacetic acid; 3-phenoxyphenyl-acetic acid; 4′-ethyl-4-biphenylcarboxylic acid; 4-isopropoxybenzoic acid; 4-methylpentanoic acid; 4-n-heptyloxybenzoic acid; 4-nitrobenzoic acid; 7-methoxy-coumarin-4-acetic acid; α-acetamidocinnamic acid; α-cyclopentylphenylacetic acid; benzoic acid; benzoylformic acid; mono-methyl cis-5-norbornene-endo-2,3-dicarboxylate; N,N-diethyl-3,6-difluorophthalamic acid; phenylacetic acid and trans-2,6-difluorocinnamic acid.
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23
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85031205085
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note
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This chemistry was undertaken using an Advanced Chemtech 396 peptide synthesizer. The average yield was 43%, based on the initial resin loading.
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24
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85031199101
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note
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During method development, compounds were characterised by NMR and LCMS. During library synthesis, compounds were analysed by LCMS before submission for biological testing.
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26
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85031199036
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note
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1=(S)-i-Pr].
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27
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18644364289
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Garofalo A.W., Wone D.W.G., Phuc A., Audia J.E., Bales C.A., Dovey H.F., Dressen D.B., Folmer B., Goldbach E.G., Guinn A.C., Latimer L.H., Mabry T.E., Nissen J.S., Pleiss M.A., Sohn S., Thorsett E.D., Tung J.S., Wu J. Bioorg. Med. Chem. Lett. 12:2002;3051.
-
(2002)
Bioorg. Med. Chem. Lett.
, vol.12
, pp. 3051
-
-
Garofalo, A.W.1
Wone, D.W.G.2
Phuc, A.3
Audia, J.E.4
Bales, C.A.5
Dovey, H.F.6
Dressen, D.B.7
Folmer, B.8
Goldbach, E.G.9
Guinn, A.C.10
Latimer, L.H.11
Mabry, T.E.12
Nissen, J.S.13
Pleiss, M.A.14
Sohn, S.15
Thorsett, E.D.16
Tung, J.S.17
Wu, J.18
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28
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85031206394
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note
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50 >75 μM).
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29
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0027172371
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See, for example:
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See, for example: Patel D.V., Rielly-Gauvin K., Ryono D.E., Free C.A., Smith S.A., Petrillo E.W. Jr. J. Med. Chem. 36:1993;2431.
-
(1993)
J. Med. Chem.
, vol.36
, pp. 2431
-
-
Patel, D.V.1
Rielly-Gauvin, K.2
Ryono, D.E.3
Free, C.A.4
Smith, S.A.5
Petrillo E.W., Jr.6
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30
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85031195350
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note
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See ref 2 and references therein.
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