Acyclic pyrazolo[3,4-d]pyrimidine nucleoside as potential leishmaniostatic agent.
A new synthesis of 6-amino-1-hydroxyethoxymethyl-4 (5H)-oxopyrazolo[3, 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.
Hasan
A
A
Division of Medicinal & Process Chemistry, Central Drug Research Institute, Lucknow, India.
Satyanarayana
M
M
Mishra
A
A
Bhakuni
D S
DS
Pratap
Ram
R
Dube
A
A
Guru
P Y
PY
D000818:Animals; D000977:Antiparasitic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006224:Cricetinae; D007893:Leishmania donovani / Q000187:drug effects*; D008297:Male; D015394:Molecular Structure; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
D000977:Antiparasitic Agents; D011741:Pyrimidine Nucleosides; C509132:acyclic pyrazolo(3,4-d)pyrimidine nucleoside