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Volumn 9, Issue 1, 2007, Pages 43-52

Combinatorial approach to N-substituted aminocyclitol libraries by solution-phase parallel synthesis and preliminary evaluation as glucocerebrosidase inhibitors

Author keywords

[No Author keywords available]

Indexed keywords

ALCOHOL DERIVATIVE; CARBAMIC ACID DERIVATIVE; CYCLOHEXANE DERIVATIVE; DRUG DERIVATIVE; ENZYME INHIBITOR; GLUCOSYLCERAMIDASE; HEXOSAMINE; IMIGLUCERASE; SULFONAMIDE; UREA;

EID: 33846649594     PISSN: 15204766     EISSN: None     Source Type: Journal    
DOI: 10.1021/cc060080o     Document Type: Article
Times cited : (21)

References (30)
  • 9
    • 0141852846 scopus 로고    scopus 로고
    • For recent examples of inositol derivatives as enzyme inhibitors, see: (a) Bashir-Uddin, Surfraz, M.; Miller, D. J.; Gani, D.; Allemann, R. K. Tetrahedron Lett. 2003, 44, 7677-7679.
    • For recent examples of inositol derivatives as enzyme inhibitors, see: (a) Bashir-Uddin, Surfraz, M.; Miller, D. J.; Gani, D.; Allemann, R. K. Tetrahedron Lett. 2003, 44, 7677-7679.
  • 20
    • 33846593505 scopus 로고    scopus 로고
    • Inositols of the chiro series 2 were obtained as racemic mixtures.
    • Inositols of the chiro series 2 were obtained as racemic mixtures.
  • 22
    • 0035132705 scopus 로고    scopus 로고
    • Building blocks were selected from among the several thousands of commercially available and in-house synthesized possibilities by generating a virtual library. The library thus obtained was filtered to remove incompatibilities with the proposed reaction pathway and classified into different families according to structural criteria. Each family was further filtered according to modified Lipinski's rules. (Tice, C. M. Pest. Manage. Sci. 2001, 57, 3-16.) Final building block selection was made by hand on the basis of structural diversity and commercial availability.
    • Building blocks were selected from among the several thousands of commercially available and "in-house" synthesized possibilities by generating a virtual library. The library thus obtained was filtered to remove incompatibilities with the proposed reaction pathway and classified into different families according to structural criteria. Each family was further filtered according to modified Lipinski's rules. (Tice, C. M. Pest. Manage. Sci. 2001, 57, 3-16.) Final building block selection was made by hand on the basis of structural diversity and commercial availability.
  • 27
    • 33846642706 scopus 로고    scopus 로고
    • The main limitation was the impossibility to avoid hydrogen losses in the standard 96-well plate format used
    • The main limitation was the impossibility to avoid hydrogen losses in the standard 96-well plate format used.
  • 28
    • 33846622908 scopus 로고    scopus 로고
    • Only library members of purity higher than 70%, according to HPLC-ELS-MS, were submitted to enzyme inhibition studies (see Supporting Information for further details).
    • Only library members of purity higher than 70%, according to HPLC-ELS-MS, were submitted to enzyme inhibition studies (see Supporting Information for further details).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.