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Volumn 13, Issue 6, 2003, Pages 1203-1206

Inhibitors of Aβ production: Solid-phase synthesis and SAR of α-hydroxycarbonyl derivatives

Author keywords

[No Author keywords available]

Indexed keywords

ALKYL GROUP; ALPHA HYDROXY KETONE DERIVATIVE; ALPHA HYDROXYCARBONYL DERIVATIVE; AMYLOID BETA PROTEIN; CARBONYL DERIVATIVE; ESTER DERIVATIVE; HYDROXYL GROUP; KETONE DERIVATIVE; PROTEIN INHIBITOR; UNCLASSIFIED DRUG; DYES, REAGENTS, INDICATORS, MARKERS AND BUFFERS; ESTER;

EID: 0037463802     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(02)01058-2     Document Type: Article
Times cited : (75)

References (30)
  • 2
    • 0035927426 scopus 로고    scopus 로고
    • (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
  • 12
    • 85031206351 scopus 로고    scopus 로고
    • 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
  • 17
    • 85031205903 scopus 로고    scopus 로고
    • See also ref 7
    • (c) See also ref 7.
  • 22
    • 85031195249 scopus 로고    scopus 로고
    • note
    • 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.
  • 23
    • 85031205085 scopus 로고    scopus 로고
    • note
    • This chemistry was undertaken using an Advanced Chemtech 396 peptide synthesizer. The average yield was 43%, based on the initial resin loading.
  • 24
    • 85031199101 scopus 로고    scopus 로고
    • note
    • During method development, compounds were characterised by NMR and LCMS. During library synthesis, compounds were analysed by LCMS before submission for biological testing.
  • 26
    • 85031199036 scopus 로고    scopus 로고
    • note
    • 1=(S)-i-Pr].
  • 28
    • 85031206394 scopus 로고    scopus 로고
    • note
    • 50 >75 μM).
  • 30
    • 85031195350 scopus 로고    scopus 로고
    • note
    • See ref 2 and references therein.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.