摘要:
N-OXIDES AND SALTS OF POLY I:POLY C WHICH ARE THEMSELVES DOUBLE-STRANDED, METHODS OF MAKING SUCH N-OXIDES AND SALTS AND PHARMACEUTICAL COMPOSITIONS THEREOF ARE DESCRIBED. THE NEW POLYI:POLY C DERIVATIVES HAVE REDUCED TOXICITY AND ARE CHARACTERIZED BY BROAD ANTIVIRAL ACTIVITY. THE METHODS COMPRISE OXIDATION WITH HYDROGEN PERIOXIDE OR A PERACID WHICH IS CONTROLLED TO AVOID SEPARATION OF THE DOUBLE-STRANDED MATERIAL INTO SINGE-STRANDED MATERIAL.
摘要:
N-OXIDES OF NATURAL DOUBLE-STANDED RIBONUCLIEC ACIDS AND SALTS THEREOF, WHICH ARE THEMSELVES DOUBLE-STRANDED, PREPARED BY REACTING DOUBLE-STRANDED RIBONUCLEIC ACIDS WITH HYDROGEN PERIOXIDE OR A PERACID, ARE DESCRIBED. THE NEW RNA DERIVATIVES ARE INTERFERON INDUCERS AND/OR HAVE ANTIVIRAL ACTIVITY AND ARE LESS TOXIC THAN THE PRENT RNA''S. NATURAL RNA''S HAVE EDENINE, CYTOSINE, URACIL AND GUANINE BASES LINKED TO REPEATING RIBOSE/PHOSPHATE BACKBONE UNITS AND DIFFERENT DEGREES OF OXIDATION OF THE BASES CAN BE CARRIED TO PRODUCE A VARIETY OF NEW N-OXIDE DERIVATIVES. THE CONVERSION TO SINGLE-STRANDED MATERIAL IS AVOIDED BY LIMITING THE EXTENT OF OXIDATION AND LEAVING SOME UNOXIDIZED BASE SITES. FORMULATION INTO AEROSOLS, INJECTIBLES AND TOPICALS IS DESCRIBED.
wherein R1 is lower alkanoyl, and R2 and R3 are each lower alkanoyl or jointly lower alkylidene are readily prepared by reaction of formic acid with corresponding starting compounds having an amino group in position 5 of the imidazole ring, and hydrogen or lower alkanoyl groups instead of each of R1, R2, R3 or alkylidene in R2 and R3. They inhibit the growth of NF sarcoma in mice.