New Inosine and Guanosine Analogs as Inhibitors of Parasitic Infections.
Abstract
A number of heterocycles and nucleosides in the pyraxolo(3,4-d)pryrimidine, pyrazolo (3,4-f)-as-triazine, s-triazolo(4,3-c)pyridine, s-triazolo(1,5-a)-striazine, imidaxo(4,5-c)pyridine and purine ring system have prepared as potential antiparasitic agents. The compounds thus synthesized were tested for their antiparasitic activities. The ED50 value for 1-beta-D-ribofuranosylpyrazolo(3,4-d)pyrimidine-4(5H)-thione is similare to that for allopurinol ribonucleoside against Leishmania amastigotes. 3-Bromo-allopurinol ribonucleoside (BK 15661) is more active than allopurinol ribnucleoside against L. tropica in vitro. 7-Deazainosine has a low ED50 dose (0.2 micrometers), but only 80% of the organism (L. tropica) were eliminated at 4 micrometers. 2-Methylinosine (BK-48428) has shown significant antitryanosomal activity (ED50 of 0.21 micrometers) 3-Deazaguanosine (BK-17405) is more active than allopurinol or allopurinol ribonucleoside aganist L. tropica in vitro (kED50 of 3.6 micrometers), and has shown significant activity against L. donovani in animals (76% suppression). Thioformycin B is also very potent agianst L donovani in vivo (87% suppression). Selenoformycin B is more active than thioformycin B, but less active thant formycin B and agianst L tropic promastigotes in vitro with an ED50 of 0.2 micrometers.
Document Details
- Document Type
- Technical Report
- Publication Date
- Nov 30, 1985
- Accession Number
- ADA164470
Entities
People
- Ganapathi R. Revankar
- Roland K. Robins
Organizations
- Brigham Young University