ChemInform Abstract: Synthesis and Radioprotective Properties of 4‐(Bis(2‐chloroethyl)amino) phenylalanyl‐L‐glutaminic Acid Derivatives.

Abstract

Synthesisand Radioprotective Properties of 4-(Bis(2chloroethyl)amino) phenylalanyl-L-glutaminic Acid Derivatives.-Reaction of the D,L-phenylalanine derivative (I) with L-glutamate (II) gives a mixture of the diethyl esters of the title phenylalanyl-L-glutaminic acid (III)/(IV). The single diastereomers, separated by column chromatography or crystallization, are transformed to the corresponding sodium salts by saponification with NaOH (cf. (V)). The esters and the salts are tested for their radioprotective properties in pure form or as a mixture of diastereomers. The best results are obtained for the mixture of sodium salts. The influence of administration scheme and time on the biological activity is discussed. -(VATULINA, G. G.; ALEKSEEVA, L. V.; ZHDANOVA, E. A.; PROKOP'EVA, I. A.; TOLSTYKH, E. I.; KRASNOV, V. P.; Khim.-Farm. Zh. 31 (1997) 5, 43-47; Inst. org. sint. Ural. otd. Ross. Akad. nauk, Ekaterinburg, Russia; RU)