Acyclic pyrazolo[3,4-d]pyrimidine nucleoside as potential leishmaniostatic agent |
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Authors: | Hasan A Satyanarayana M Mishra A Bhakuni D S Pratap Ram Dube A Guru P Y |
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Affiliation: | Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow, India. |
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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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