Synthesis and antileishmanial activity of some 1- or 2-(dihydroxyalkyl) and 3-(dihydroxyalkoxy)pyrazolo [3,4-d] pyrimidines.
Several new derivatives of 4-amino-, 4,6-diamino- and 4-hydrazino-[3,4-d]pyrimidine dihydroxyalkyl substituted in the 1 or 2 positions, or dihydroxyalkoxy substituted in the 3 position have been synthesized. Some of these compounds were evaluated for their activity against Leishmania infantum in mice. The highest degree of antileishmanial activity was displayed by the 4-amino-1-(dihydroxyalkyl) derivatives which yielded parasite inhibition values nearly comparable with that of glucantime in a standard 5-day test.
Gatta
F
F
Laboratorio di Chimica del Farmaco, Instituto Superiore di Sanità, Roma.
Gradoni
L
L
Lupardini
E
E
Gramiccia
M
M
Orsini
S
S
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis*; D007279:Injections, Subcutaneous; D007893:Leishmania donovani / Q000187:drug effects*; D007898:Leishmaniasis, Visceral / Q000188:drug therapy* / Q000469:parasitology; D008536:Meglumine / Q000494:pharmacology; D000077485:Meglumine Antimoniate; D051379:Mice; D008807:Mice, Inbred BALB C; D009942:Organometallic Compounds / Q000494:pharmacology; D011720:Pyrazoles / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D011743:Pyrimidines / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000981:Antiprotozoal Agents; D009942:Organometallic Compounds; D011720:Pyrazoles; D011743:Pyrimidines; D008536:Meglumine; D000077485:Meglumine Antimoniate