Abstract |
Strains of Trypanosoma cruzi differ in their susceptibilities to and metabolism of pyrazolopyrimidines. Allopurinol riboside can control but not eliminate infections with a sensitive strain in both tissue culture and mice. Formycin B, which proved to be greater than 10-fold more effective on a weight basis, showed a similar strain specificity but could eliminate an infection with a sensitive strain from tissue culture. However, this drug, unlike allopurinol riboside, was converted to toxic analogues of adenosine mono-, di-, and triphosphate by uninfected tissue culture cells. Thiopurinol and its riboside were effective against all strains unless culture was performed in purine-defined medium. Thus formycin B and allopurinol riboside appear to be good models for the design of antitrypanosomal agents. Suitable modification of the molecule may provide an effective chemotherapeutic agent.
|
Authors | R L Berens, J J Marr, D L Looker, D J Nelson, S W LaFon |
Journal | The Journal of infectious diseases
(J Infect Dis)
Vol. 150
Issue 4
Pg. 602-8
(Oct 1984)
ISSN: 0022-1899 [Print] United States |
PMID | 6436394
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Research Support, U.S. Gov't, P.H.S.)
|
Chemical References |
- Antiprotozoal Agents
- Formycins
- Ribonucleosides
- Thionucleosides
- formycin B
- 4-aminopyrazolo(3,4-d)pyrimidine
- thiopurinol ribonucleoside
- Inosine
- Allopurinol
- tisopurine
- Adenine
- allopurinol riboside
|
Topics |
- Adenine
(analogs & derivatives, pharmacology)
- Allopurinol
(analogs & derivatives, pharmacology)
- Animals
- Antiprotozoal Agents
(pharmacology, therapeutic use)
- Chagas Disease
(drug therapy)
- Drug Resistance
- Formycins
(metabolism, pharmacology)
- Inosine
(metabolism)
- Mice
- Mice, Inbred DBA
- Ribonucleosides
(pharmacology)
- Thionucleosides
(pharmacology)
- Trypanosoma cruzi
(drug effects, metabolism)
|