Synthesis and Biological Evaluation of Brain-Specific Anti-RNA Viral Agents
Abstract
Ribavirin is a potentially useful drug for treating encephalitic disease but is excluded from the brain because of its poor membrane permeability. This contract has attempted to develop brain-targeted delivery forms of ribavirin in an attempt to increase its efficacy towards central maladies. Ten such delivery systems have been prepared. These include several in which a brain-selective 1,4-dihydrotrigonellinate was attached to the 5'- position, one in which the 2'-position was modified and several others. After preparation, analytical systems were developed to separate, detect and quantitate these materials both in vivo and in vitro. The stability of selected compounds was then studied in various biological matrices. Further in vivo testing included tissue distribution studies and antiviral activity studies performed in a murine viral encephalitic model. Ribavirin, Brain, Targeted delivery, RNA viruses, Dihydropyridines, Punta Toro virus, RA I, Pharmacology, Pathogenic materials, Polypeptide, Deoxyribonucleic acids (DNA), Labial and genital herpes, Lassa fever, Dengue fever, Chicken pox, Shingles, Mononucleosis, 1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin), Riboside, 1- methyl-1,4-dihydronicotinated moiety.
Document Details
- Document Type
- Technical Report
- Publication Date
- Mar 31, 1990
- Accession Number
- ADA221238
Entities
People
- Marcus E. Brewster