126399-19-7Relevant articles and documents
PREPARATION AND CHARACTERIZATION OF NEW ANALOGUES OF DALARGIN
Pospisek, Jan,Barth, Tomislav,Bespalova, Zhanna D.,Titov, Mikhail I.,Maskova, Hana P.,et al.
, p. 2271 - 2275 (2007/10/02)
Tert-butyloxycarbonyl-O-tert-butyloxycarbonyl-L-tyrosyl-D-alanyl-glycyl-L-phenylalanyl-DL-neopentylglycyl-L-arginine was prepared by means of fragment condensation in solution.Protecting groups were removed with trifluoroacetic and the diastereoisomeric peptides were separated employing high-performance liquid chromatography (HPLC) and the absolute configuration of neopentylglycine in each diastereomer was determined by two different methods: analysis of enzymatic degradation with carboxypeptidaseB and 1H NMR spectroscopic data.The hexapeptide with L-neopentylglycine in position 5 exhibited a 20 times higher activity in a standard test on isolated guinea-pig ileum (GPI).The hexapeptide with D-neopentylglycine in position 5 exhibited a 4 times higher activity than Dalargin in the GPI test but its effect was prolonged in comparison to the analog with L-neopentylglycine and Dalargin.