Abstract: | Essentially pure (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]-diazepin-8-ol and the process for the production of (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol by inoculating an aqueous nutrient medium, preferably containing sources of assimilable carbon and nitrogen and added inorganic salt and having a pH between about 6 and 8, with a (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol producing strain of Streptomyces antibioticus, such as the strain corresponding to NRRL 3238, conducting a fermentation under aseptic aerobic conditions at a temperature between about 20 and 45.degree.C. until a substantial quantity of (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo- [4,5-d][1,3]diazepin-8-ol is formed, and isolating the desired product from the fermentation mixture are disclosed. The (R)-3-(2-deoxy-.beta.-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[ 4,5-d][1,3]diazepin-8-ol potentiates the activity of 9-(.beta.-D-arabinofuranosyl)adenine as an antiviral agent that is active in vitro and in vivo against DNA viruses such as herpes and vaccinia viruses. |
Inventor(s): | Ryder; Albert (Detroit, MI), Dion; Henry W. (Detroit, MI), Woo; Peter W. (Ann Arbor, MI), Howells; John D. (Grosse Pointe Woods, MI) |