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Volumn 20, Issue 3, 2010, Pages 1173-1176

Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists

Author keywords

[No Author keywords available]

Indexed keywords

AMINE; CYTOCHROME P450 3A4; DIPEPTIDE; ESTER; HETEROARYLAMINE; HETEROCYCLIC COMPOUND; HYDROXYPROLINE METHYL ESTER; PIPERIDINE; PIPERIDINE DERIVATIVE; PRODRUG; PROLINE DERIVATIVE; PROLINE DIPEPTIDE; PROTEIN INHIBITOR; TERTIARY AMINE; UNCLASSIFIED DRUG; VERY LATE ACTIVATION ANTIGEN 4; VERY LATE ACTIVATION ANTIGEN 4 RECEPTOR; VLA 4 ANTAGONIST; PROLINE; PROTEIN BINDING;

EID: 74049161233     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.12.009     Document Type: Article
Times cited : (7)

References (23)
  • 18
    • 84925561039 scopus 로고    scopus 로고
    • note
    • -1.
  • 19
    • 0034685213 scopus 로고    scopus 로고
    • For discussions on the regioselectivity of 1,2,4-triazole and tetrazole alkylation, see:
    • For discussions on the regioselectivity of 1,2,4-triazole and tetrazole alkylation, see:. Bulger P.G., Cottrell I.F., Cowden C.J., Davies A.J., and Dolling U.-H. Tetrahedron Lett. 41 (2000) 1297
    • (2000) Tetrahedron Lett. , vol.41 , pp. 1297
    • Bulger, P.G.1    Cottrell, I.F.2    Cowden, C.J.3    Davies, A.J.4    Dolling, U.-H.5
  • 21
    • 84925561038 scopus 로고    scopus 로고
    • note
    • We have previously demonstrated that this class of compounds generally has a higher affinity for the activated state of VLA-4. Thus, potency was examined only against the resting state of VLA-4 to best differentiate compounds.
  • 22
    • 84925567483 scopus 로고    scopus 로고
    • note
    • 125I]-tracer shown below was utilized to assess binding potency, receptor off-rate, and rat receptor occupancy. A detailed description of each of these experiments was recently provided in the Supplementary data of Ref. 8.{A figure is presented}


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.