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Volumn 21, Issue 1, 2011, Pages 307-310

Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists

Author keywords

Amino acid; (S) 2,3 Diaminopropanoic acid replacement; LFA 1 ICAM 1 antagonist; Structure activity relationship; Tetrahydroisoquinoline

Indexed keywords

2,3 DIAMINOPROPANOIC ACID; ALPHA AMINO ACID; INTERCELLULAR ADHESION MOLECULE 1; LYMPHOCYTE FUNCTION ASSOCIATED ANTIGEN 1; PROPIONIC ACID; TETRAHYDROISOQUINOLINE; UNCLASSIFIED DRUG;

EID: 78650516916     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.11.014     Document Type: Article
Times cited : (19)

References (47)
  • 1
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    • 78650516452 scopus 로고    scopus 로고
    • note
    • 2 solution. Samples were taken at 0, 30, and 60 min three time points and tested on LC/MS. The data were reported as a ratio of the peak area at 30 min or 60 min relative to the one at 0 min. Lidocaine and Dextromethorphan were used as positive controls. 1p: 92% at 30 min in human liver microsomes (HLM); 1v: >95% at 30 min in rat liver microsomes (RLM) and 86% at 30 min in HLM; and 1y: >65% at 30 min in RLM and >95% at 30 min in HLM.
  • 47
    • 78650512237 scopus 로고    scopus 로고
    • note
    • In general, analogs bearing the 'right-wing' amino acid moiety of 1y and various 'left-wing' residues show better potency relative to the corresponding DAP analogs in either the Hut-78 or Staphylococcal Enterotoxin B (SEB)-stimulated T-cell activation assay in the presence of either human or fetal bovine serum. The data are not shown.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.