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1 February 2000 A Chlorodiazirine Analog of Pentamidine with Anti-Trypanosomal Activity
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Abstract

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.

Alfred C. Nichols, K. Lemone Yielding, and Samuel A. O. Agbe "A Chlorodiazirine Analog of Pentamidine with Anti-Trypanosomal Activity," Journal of Parasitology 86(1), (1 February 2000). https://doi.org/10.1645/0022-3395(2000)086[0177:ACAOPW]2.0.CO;2
Published: 1 February 2000
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