DEVELOPMENT OF NEW NONPEPTIDE GPIIB IIIA ANTAGONISTS, NSL-95315 AND NSL-95317, ISOSTERES OF NSL-95300/

Authors
ASARI T ISHIKAWA S SASAKI T KATADA J HAYASHI Y HARADA T YANO M YASUDA E UNO I OJIMA I
Citation
T. Asari et al., DEVELOPMENT OF NEW NONPEPTIDE GPIIB IIIA ANTAGONISTS, NSL-95315 AND NSL-95317, ISOSTERES OF NSL-95300/, Bioorganic & medicinal chemistry letters, 7(16), 1997, pp. 2099-2104
Citations number
17
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
16
Year of publication
1997
Pages
2099 - 2104
Database
ISI
SICI code
0960-894X(1997)7:16<2099:DONNGI>2.0.ZU;2-K
Abstract
The synthetic and structure-activity relationship (SAR) studies of new non-peptide GPIIb/IIIa antagonists (1a-f and 3) were conducted by rep lacing one amide bond of NSL-95300 (2) with an (E)-double bond or an e none group. NSL-95315 (1a) and NSL-95317 (3) showed the inhibitory act ivity for collagen-induced human platelet aggregation with IC50 values of 0.25 mu M and 0.21 mu M, respectively. (C) 1997 Elsevier Science L td.