To obtain the subject new compound capable of inhibiting the bond between leukocyte and ICAM-I playing a central role among cell adhesion molecules and useful as e.g. an excellent immunosuppressive agent.
This compound is expressed by formula I [R1 is H or a 1-4C alkyl; X is O or a (substituted) amino; Y is a (substituted) benzene or 1,3-thiazole ring; Z is e.g. (CH2)n ((n) is 0 to 3) or CH=CH; R2 is a (substituted) 1-4C alkyl or a (substituted) phenyl; and R3 is e.g. H or a (substituted) piperazine ring], e.g. 3-[4-(benzothiazol-2-yl)aminobenzoyl]aminopropionic acid ethyl ester. The compound is obtained by condensing a compound of formula III with a compound of formula II (R4 is hydroxy or a halogen) in the presence of an organic base e.g. triethylamine in a solvent of e.g. methylene chloride at 0°C to room temperature.
NOMURA MASAHIRO
SAWADA TAKAYUKI
KONO YASUSHI
SEKOE YASUHIKO