| abstract |
N-aroylphenylalanine derivatives, which comprise the formula Ien where one of X and X is H, halogen or lower alkyl and the other is a group of formula X-6in where: R1 is hydrogen or lower alkyl, R15 is hydrogen, halogen, nitro, lower alkylsulfonyl, cyano, lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxyl, lower alkylaminosulfonyl, lower perfluoralkyl, lower alkylthio, lower hydroxyalkyl, lower alkoxy lower alkyl, lower alkylthio, lower alkylsilyl, lower alkylsilyl, lower alkylsilyl, lower alkylsilyl , aroyl, aryl or a group of formula R17-C ::: C, R16 is H, halogen, nitro, cyano, lower alkyl, OH, lower perfluoralkyl or lower alkyl, and R17 is H, aryl, heteroaryl, or lower alkyl which is unsubstituted or substituted with OH, aryl or heteroaryl, is already 0 or 1; or one of X and X is a group of X-7 deformula in which Het is a heteroaromatic ring of 5 or 6 members containing 1, 2 or 3 heteroatoms selected from N, O and S; or Het is a 9 or 10-membered bicyclic heteroheromatic ring, which contains 1, 2, 3 or 4 heteroatoms selected from O, S and N; a, R1, R15 and R16 are as defined for X-6 and R30 is hydrogen or lower alkyl, or does not exist; or one of X and X is a group of formula X-10 wherein R18 is hydrogen, substituted lower alkyl or unsubstituted, aryl, heteroaryl, arylalkyl, or heteroarylalkyl, R19 is unsubstituted or substituted lower alkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl, and R20 is unsubstituted or substituted lower alkyl, lower alkanoyl, optionally substituted with carboxyl, aroyl or aryloxy; and Y is a group of formula Y-1 wherein R22 and R23 are independently aryl, heteroaryl or lower alkyl which is unsubstituted or substituted with one or more chloro, bromine, nitro, hydroxy, lower alkoxy, aryl, lower alkanoyl, aroyl or cyano, R24 is aryl, cyano, alkylsulfonyl or alkyl or lower or alkenyl unsubstituted or substituted with an aryl or heteroaryl ring, and when R22 is aryl and R23 is aryl or lower alkyl, R24 is H, and the total number of |