SYNTHESIS OF FUNCTIONALIZED PYRAZOLES AND PYRAZOLO[3,4-D]PYRIMIDINES AS POTENTIAL LEISHMANICIDES

Various methylthio-3-piperazinylacrylonitriles/arcylamides (2a-k) have been synthesized by the reaction of ketene dithioacetals (1a,b) with substituted piperazines. Reaction of 2a-i with hydrazine hydrate affor ds the respective pyrazoles (3a-i) which on boiling in formamide provi de the pyrazolo[3,4-d]pyrimidines (4a-g). Reaction of oxy-3-methylthio -1H-pyrazol-5-yl)-3-phenylthiourea (5) with hydrazine hydrate affords io-6-phenylamino-1H-pyrazolo[3,4-d]pyrimidin-4-one (6). Some of the co mpounds have been screened for their in vitro leishmanicidal activity.