التفاصيل البيبلوغرافية
العنوان:
Aminoisoquinolines: Design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA
المؤلفون:
Mason Helen J , Karen D. Brown , Valeria Chu , Guyan Liang , Daniel M. Green , Alfred P. Spada , Henry W. Pauls , Ross Bentley , Cuong Ly , Roderick S. Davis , Dennis J. Colussi , Daniel L. Cheney , Michael R. Becker , Y.M. Choi-Sledeski , Christopher T. Dunwiddie , Robert J. Leadley , Ewing William R , John H. Barton
المصدر:
Bioorganic & Medicinal Chemistry Letters . 9:2539-2544
بيانات النشر:
Elsevier BV, 1999.
سنة النشر:
1999
مصطلحات موضوعية:
Serine Proteinase Inhibitors , medicine.drug_mechanism_of_action , Isostere , Stereochemistry , Clinical Biochemistry , Factor Xa Inhibitor , Administration, Oral , Pharmaceutical Science , Biochemistry , Chemical synthesis , Benzamidine , Amidine , Serine , Structure-Activity Relationship , chemistry.chemical_compound , Dogs , Drug Discovery , medicine , Animals , Structure–activity relationship , Molecular Biology , Binding Sites , Organic Chemistry , Isoquinolines , Benzamidines , chemistry , Molecular Medicine , Factor Xa Inhibitors
الوصف:
The design, synthesis and SAR of sulfonamidopyrrolidinone fXa inhibitors incorporating a new benzamidine isostere, namely aminoisoquinolines, is described. These inhibitors have higher Caco-2 cell permeability than comparable benzamidines and attain higher levels of exposure upon oral dosing. The most potent member 14b (fXa Ki=6 nM) is selective against other serine proteases of interest (>600 fold).
تدمد:
0960-894X
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a71de730d502044d956f73b19dd821f https://doi.org/10.1016/s0960-894x (99)00421-7
حقوق:
CLOSED
رقم الأكسشن:
edsair.doi.dedup.....8a71de730d502044d956f73b19dd821f
قاعدة البيانات:
OpenAIRE
