PURPOSE: To obtain a new modified oligodeoxyribonucleotide, having specific dyscratic activities against AIDS virus and useful for preventing and treating AIDS diseases.
CONSTITUTION: This compound of formula I [Q is R1 to R3 or Z (R1 to R3 are each H, a 1-4C alkyl, an aryl, etc.; Z is C, Si, etc.); R4 is H, a (substituted) 1-4C alkyl, a (substituted) aryl, etc.; Y1, Y3 and Y4 are each 0, S or NH; Y2 is O, S, NH, a 1-4C alkylene or phenylene; X is a (OH-substituted) 1-10C alkylene; (n) and (m) are each 0-10; B is an oligodeoxyribonucleotide in which a phosphodiester group having 3-9 chain length is partially converted into a phosphorothioate type diester, etc.], e.g. a compound of formula II. Furthermore, the compound of formula I is obtained by reacting, e.g. a compound of formula III (D' is a base of a nucleotide having amino group protected with an acyl group on the 5'-terminal side; V is a protecting group of a phosphoric acid part; U is amino group in an amidite part) with a compound of formula IV [F is an oligonucleotide part after removing one nucleotide on the 5'-terminal side of an effective base sequence; W1 is a controlled pore glass(CPG) to the oxygen atom of the 3'-hydroxyl group in the 3'-terminal part of the oligonucleotide F in the final objective compound].
KOGA RIKA
HOTODA HITOSHI
KANEKO MASAKATSU
OMINE HISANORI
FURUKAWA HIDEHIKO
NISHIGAKI TAKASHI
