New Inosine and Guanosine Analogs as Inhibitors of Parasitic Infections.
Annual rept. 1 Feb 84-30 Nov 85, Final rept. 1 Sep 82-30 Nov 85,
BRIGHAM YOUNG UNIV PROVO UT
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A number of heterocycles and nucleosides in the pyraxolo3,4-dpryrimidine, pyrazolo 3,4-f-as-triazine, s-triazolo4,3-cpyridine, s-triazolo1,5-a-striazine, imidaxo4,5-cpyridine 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-ribofuranosylpyrazolo3,4-dpyrimidine-45H-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.