A chlorodiazirine derivative of pentamidine was synthesized and tested for anti-trypanosomal activity using EATRO stock 164 trypanosomes in cell culture. Anti-trypanosomal activity was measured as a decrease in [3H]hypoxanthine incorporation by the organisms. The derivative, 3,3′-[1,5-pentanediylbis(oxy-4,1-phenylene)]bis(3-chloro-3H-diazirine), at a treatment level of 0.1 µM inhibited isotope incorporation by 40–50% compared to nontreated controls. At this concentration, pentamidine inhibited incorporation only 10–15%. The derivative is a nonionic molecule with much different solubility properties than the parent compound and should readily cross the blood–brain barrier.
A Chlorodiazirine Analog of Pentamidine with Anti-Trypanosomal Activity
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Alfred C. Nichols, K. Lemone Yielding, Samuel A. O. Agbe; A Chlorodiazirine Analog of Pentamidine with Anti-Trypanosomal Activity. J Parasitol 1 February 2000; 86 (1): 177–180. doi: https://doi.org/10.1645/0022-3395(2000)086[0177:ACAOPW]2.0.CO;2
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