A four component coupling strategy for the synthesis of D-phenylglycinamide-derived non-covalent factor Xa inhibitors.
A novel isonitrile derivative was synthesized and used in an Ugi four component coupling reaction to explore aryl group substitution effects on inhibition of the coagulation cascade serine protease factor Xa.
Sheehan
Scott M
SM
Lilly Research Laboratories, A Division of Eli Lilly and Company, IN 46285, Indianapolis, USA. sheehan_scott@lilly.com
Masters
John J
JJ
Wiley
Michael R
MR
Young
Stephen C
SC
Liebeschuetz
John W
JW
Jones
Stuart D
SD
Murray
Christopher W
CW
Franciskovich
Jeffrey B
JB
Engel
David B
DB
Weber
Wayne W
WW
Marimuthu
Jothirajah
J
Kyle
Jeffrey A
JA
Smallwood
Jeffrey K
JK
Farmen
Mark W
MW
Smith
Gerald F
GF
D065427:Factor Xa Inhibitors; D005998:Glycine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D065427:Factor Xa Inhibitors; D007202:Indicators and Reagents; D015842:Serine Proteinase Inhibitors; C470025:phenylglycinamide; D005998:Glycine