SYNTHESIS OF SOME 1-(DIHYDROXYPROPYL)PYRAZOLO[3,4-D]-PYRIMIDINES AND INVIVO EVALUATION OF THEIR ANTILEISHMANIAL AND ANTITRYPANOSOMAL ACTIVITY

A number of 1-(2,3-dihydroxypropyl)- and 1-[2-(1,3-dihydroxypropyl)]pyrazolo[3,4-d]pyrimidines were synthesized. Some of these compounds were evaluated for their activity against Leishmania infantum and Trypanosoma brucei brucei in mice. The highest degree of antileishmanial activity was displayed by the 4-amino-1-(RS)-(2,3-dihydroxypropylpyrazolo[3,4-d]pyrimidine 11a, which yielded a 87% and 96% parasite inhibition in a standard 5-day test and in a long-term (14 days) treatment, respectively, though full cures of animals were not achieved. On the contrary, this derivative did not significantly prolong the survival of T b brucei infected mice. © 1990.