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Acyclic pyrazolo[3,4-d]pyrimidine nucleoside as potential leishmaniostatic agent
Authors:Hasan A  Satyanarayana M  Mishra A  Bhakuni D S  Pratap Ram  Dube A  Guru P Y
Affiliation:Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow, India.
Abstract:A new synthesis of 6-amino-1-hydroxyethoxymethyl-4 (5H)-oxopyrazolo3, 4-d]pyrimidine (4) has been mentioned. Compound 4 exhibited inhibition of amastigotes of Leishmania donovani to the extent of 89 % at 30 microg/mL, whereas iso-guanine analogue 5 had the inhibition only to the extent of 52.8% at 100 microg/mL in vitro. In hamster model the maximum inhibitory response for compound 4 against amastigotes multiplication was observed to be 94% at 50 mg/kg single dose for 5 consecutive days.
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