A. Tanaka et al., DESIGN, SYNTHESIS, AND EVALUATION OF ORALLY-ACTIVE FIBRINOGEN INHIBITORS, Bioorganic & medicinal chemistry letters, 7(5), 1997, pp. 521-526
Low molecular weight and orally active fibrinogen inhibitors are descr
ibed. The compounds studied in this work were rationally designed base
d on a metabolic study of a peptidic fibrinogen inhibitor, 4-(4-amidin
ophenoxy)butanoylaspartylvaline (1, FK633), which led to the synthesis
of a potent and orally active antiplatelet agent, amidinophenoxy)buta
noylaspartylvalylthiomorpholine 1,1-dioxide (3 f, FR158999). (C) 1997
Elsevier Science Ltd.