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Structure-activity relationships of pentamidine analogs against Giardia lamblia and correlation of antigiardial activity with DNA-binding affinity

C. A. Bell, M. Cory, T. A. Fairley, R. R. Tidwell, J. E. Hall
1991

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1,5-Di(4-amidinophenoxy)pentane (pentamidine) and 38 analogs of pentamidine were screened for in vitro activity against the enteric protozoan Giardia lamblia WB (ATCC 30957). All compounds were active against G. lamblia as measured by a [methyl-3H]thymidine incorporation assay. Antigiardial activity varied widely, with 50 % inhibitory concentrations (IC50s) ranging from 0.51 ± 0.13 μM (mean ± standard deviation) for the most active compound to over 100.0 μM for the least active compounds. The
more » ... 50of the most potent antigiardial agent.1,5-Di(4-amidinophenoxy)pentane (pentamidine) and 38 analogs of pentamidine were screened for in vitro activity against the enteric protozoan Giardia lamblia WB (ATCC 30957). All compounds were active against G. lamblia as measured by a [methyl-3H]thymidine incorporation assay. Antigiardial activity varied widely, with 50 % inhibitory concentrations (IC50s) ranging from 0.51 ± 0.13 μM (mean ± standard deviation) for the most active compound to over 100.0 μM for the least active compounds. The IC50of the most potent antigiardial agent.
doi:10.17615/na14-mv68 fatcat:zf4h3q5rvff2vjrwnsianvhegm
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C. A. Bell, M. Cory, T. A. Fairley, R. R. Tidwell, J. E. Hall. "Structure-activity relationships of pentamidine analogs against Giardia lamblia and correlation of antigiardial activity with DNA-binding affinity." (1991)