SPERGUALIN ANALOG AND ITS USE
PURPOSE:To obtain a new compound having low toxicity, chemical stability and excellent immunosuppressive action. CONSTITUTION:A compound of the formula GU-X1-(CH2)a-CONH-X2- CONH-(CH2)4-NH-(CH2)3-NH-Y [Gu is guanidino; X1 is (CH2)5 or phenylene; (a) is 4-13; (X2 is (CH2)0-2-CH(R00)0-2; R00 is H, OH,...
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Zusammenfassung: | PURPOSE:To obtain a new compound having low toxicity, chemical stability and excellent immunosuppressive action. CONSTITUTION:A compound of the formula GU-X1-(CH2)a-CONH-X2- CONH-(CH2)4-NH-(CH2)3-NH-Y [Gu is guanidino; X1 is (CH2)5 or phenylene; (a) is 4-13; (X2 is (CH2)0-2-CH(R00)0-2; R00 is H, OH, OCH3 or CH2OH; Y is H or a residue after removal of OH from carboxyl of an amino acid or a peptide] or its salt such as 10-{N-(11-guanidinoundecanoyl)-r-amino-beta- hydroxybutanoyl}-1,5,10-triazadecane. The compound is obtained by removing a protecting group of a compound of the formula Gu-X1-(CH2)a-CONH-X2- CONH-(CH2)4-NR1-(CH2)3-NH-R2-R2 by reduction, acidolysis, hydrolysis, etc. The compound is useful for suppressing rejection in organ transplantation and skin graft and treating autoimmune diseases such as multiple sclerosis, hemolytic anemia, etc. |
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