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Volumn 17, Issue 21, 2007, Pages 5790-5795

Amino-caprolactam derivatives as γ-secretase inhibitors

Author keywords

Secretase inhibitors; Alzheimer's disease; N Benzyl amino caprolactams

Indexed keywords

AMINOCAPROLACTAM DERIVATIVE; AMYLOID BETA PROTEIN; AMYLOID BETA PROTEIN[1-40]; AMYLOID BETA PROTEIN[1-42]; AMYLOID PRECURSOR PROTEIN; CYTOCHROME P450 2C19; CYTOCHROME P450 3A4; GAMMA SECRETASE INHIBITOR; SULFONAMIDE; UNCLASSIFIED DRUG;

EID: 34548858715     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.08.047     Document Type: Article
Times cited : (13)

References (15)
  • 7
    • 34548814581 scopus 로고    scopus 로고
    • note
    • 50 values determined using curve fitting in CurveMaster (Excel-Fit based data analysis package). Also, 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.
  • 8
    • 34548834844 scopus 로고    scopus 로고
    • Roberts, S. B.; Hendrick, J. P.; Vinitsky, A.; Lewis, M.; Smith, D. W.; Pak, R. Isolation of functionally active γ-secretase presenilin 1 complex and fluorescence assay for γ-secretase activity and inhibitors. US 2004, 0121411 A1.
  • 9
    • 34548823908 scopus 로고    scopus 로고
    • Purchased from ComGenex Corporation as part of a collection of sulfonamides.
  • 10
    • 34548862718 scopus 로고    scopus 로고
    • Recently disclosed in a patent, Martin, N.; preparation of N-substituted heterocyclic sulfonamides for treating cognitive disorders. US 2006/0270657A1.
  • 12
    • 34548820033 scopus 로고    scopus 로고
    • note
    • The 3 amino-2-piperidone was synthesized from d-ornithine following the method of Pellegata (9). The 3-amino-2-pyrrolidinone was purchased from Ramidus AB.
  • 13
    • 34548830916 scopus 로고    scopus 로고
    • note
    • Possible clarifications for the 10-fold increase in activity include but are not limited to: antagonism or partial agonist activity by the inactive enantiomer, chiral ligand regulated enzyme activity, allosteric binding by one of the enantiomers or even relative error in the binding assay. These hypothetical explanations are being explored further.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.