Action of pyrazolopyrimidine derivatives on Trypanosoma rangeli culture forms

• Published in: Comparative biochemistry and physiology. C, Comparative pharmacology Vol. 83; no. 2; pp. 291 - 294
• Main Authors: Avila, JoséLuis, Polegre, María A., Robins, Roland K.
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier B.V 1986; New York, NY Pergamon Press
• Subjects: Animals; Biochemistry. Physiology. Immunology. Molecular biology; Biological and medical sciences; Fundamental and applied biological sciences. Psychology; Protozoa; Pyrimidines - pharmacology; Structure-Activity Relationship; Trypanocidal Agents - pharmacology; Trypanosoma - drug effects; Trypanosoma rangeli; Cell proliferation; Rhizoflagellata; Protozoa; Antiprotozoal agent; Cell culture; Inhibition
• ISSN: 0306-4492; 0742-8413
• DOI: 10.1016/0742-8413(86)90125-8

1. The capacity of 54 different pyrazolo(3,4- d)- or pyrazolo(4,3- d)pyrimidine derivatives to inhibit the multiplication of Trypunosoma rangeli culture forms was evaluated. 2. Among pyrazolo(3,4- d)pyrimidines, 14 derivatives showed trypanostatic activity, 4-aminopyrazolo(3,4- d) pyrimidine (APP) being the most active, with 4-hydroxypyrazolo(3,4- d)pyrimidine (HPP) lacking trypanostatic activity. 3. 7-Hydroxy-3-β- d-ribofuranosylpyrazolo(4,3- d)pyrimidine (FoB) was as active as 7-amino-3-β- dribofuranosylpyrazolo(4,3- d) pyrimidme (FoA), both compounds being five-fold less inhibitory than APP. 4. It can be concluded that, regarding T. rangeli, the chemical analogy to hypoxanthine or inosine of pyrazolo(3,4- d)- and pyrazolo(4,3- d)pyrimidine, respectively, is not absolutely critical, as different modifications on the heterocyclic ring did not abolish the inhibitory activity of these compounds.