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Volumn 21, Issue 5, 2011, Pages 1536-1540

Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors

Author keywords

Anticoagulant; Inhibitor; Thrombin

Indexed keywords

ACETAMIDE DERIVATIVE; AMINOPYRIDINONEACETAMIDE; BENZAMIDE; BENZAMIDE DERIVATIVE; BENZENE DERIVATIVE; DIPHENYL ETHER; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

EID: 79951723419     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.12.105     Document Type: Article
Times cited : (6)

References (19)
  • 6
    • 0032493412 scopus 로고    scopus 로고
    • Our involvement in this series was initiated based solely on the structures disclosed in the original patent applications in ref 2 above. After the work commenced, more information about compound 3 specifically (including its thrombin potency) and this series in general, was published. See: T. Lu, B. Tomczuk, C.R. Illig, R.F. Bone, L. Murphy, J. Spurlino, F.R. Salemme, and R.M. Soll Bioorg. Med. Chem. Lett. 8 1998 1595
    • (1998) Bioorg. Med. Chem. Lett. , vol.8 , pp. 1595
    • Lu, T.1    Tomczuk, B.2    Illig, C.R.3    Bone, R.F.4    Murphy, L.5    Spurlino, J.6    Salemme, F.R.7    Soll, R.M.8
  • 18
    • 79951722780 scopus 로고    scopus 로고
    • We consider human plasma 2 × APTT values of 1 μM or less to be generally predictive of good in vivo efficacy with lower concentrations being predictive of greater efficacy. We use this 1 μM mark routinely as a gate for determining whether to evaluate a compound further in vivo in the rat ferric chloride efficacy assay (see Ref. 4). In practice, in optimizing compounds, we strive to achieve 2 × APTT values of <0.5 μM
    • We consider human plasma 2 × APTT values of 1 μM or less to be generally predictive of good in vivo efficacy with lower concentrations being predictive of greater efficacy. We use this 1 μM mark routinely as a gate for determining whether to evaluate a compound further in vivo in the rat ferric chloride efficacy assay (see Ref. 4). In practice, in optimizing compounds, we strive to achieve 2 × APTT values of <0.5 μM.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.