1,4-Bis(4-guanylphenylethyl)benzenes as potential antitrypanosomal agents.

doi:10.1002/JPS.2600710426

Paper

1,4-Bis(4-guanylphenylethyl)benzenes as potential antitrypanosomal agents.

Published Apr 1, 1982 · B. Das, V. B. Zalkow, M. Forrester

Journal of pharmaceutical sciences

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4

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Abstract

A series of 1,4-bis(4-guanylphenylethyl)benzenes, including masked amidines in which the guanyl function is incorporated into a heterocyclic ring, were prepared for screening as potential antitrypanosomal agents. Some of these compounds were active against Trypanosoma rhodesiense in mice. The diamidines were prepared by standard methods from 1,4-bis(4-cyanophenylethyl)benzene which was obtained from 1,4-bis(4-cyanostyryl)benzene by diimide reduction. The latter compound was prepared by the Wittig reaction between 4-cyanobenzylphosphonium ylide and terephthaldicarboxaldehyde.

Study Snapshot

1,4-bis(4-guanylphenylethyl)benzenes show potential as antitrypanosomal agents, with some showing activity against Trypanosoma rhodesiense in mice.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

1,4-Bis(4-guanylphenylethyl)benzenes as potential antitrypanosomal agents.

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References

Synthesis and antitrypanosomal activity of some bis(4-guanylphenyl) five- and six-membered ring heterocycles.

Bis(4-guanylphenyl) compounds show good antitrypanosomal activity without acute toxicity, with 2,5-bis(4-guanylphenyl)-1,3-oxazole and -1,3,4-thiadiazole showing comparable activity to stilbamidine and pen

Synthesis and antiprotozoal activity of 2,5-bis(4-guanylphenyl)furans.

2,5-bis(4-guanylphenyl)furans show promising antitrypanosomal activity, with six compounds showing curative effects in mice at submilligram dosage levels, outperforming stilbamidine, hydroxystilbamidine, and pentamidine.

Screening large numbers of compounds in a model based on mortality of Trypanosoma rhodesiense infected mice.

This study developed a test system to evaluate trypanosomicidal activity of large numbers of candidate drugs, identifying over 6% active compounds among over 5,500 tested.

Citations

Synthesis and trypanocidal activity of the bis-carba analogue of pentamidine

The bis-carba analogue of pentamidine, while 20-fold less active against Trypanosoma brucei infection in mice, does not undergo oxidative cleavage, suggesting a new direction for designing less toxic pentamidine analogues.