THE ACTION OF SUBSTANCES ANALOGOUS TO DIAMINODIPHENOXYALKANES AGAINST SCHISTOSOMA MANSONI

Abstract

The effects on activity against Schistosoma mansoni of further modifications of the diaminodiphenoxyalkanes are reported. Replacement of the amino‐group by any of a large number of other groups destroys activity. Activity is retained in the presence of certain substituted (hydroxyalkyl, carboxyalkyl) amino‐groups and in some of their aldehyde‐bisulphite derivatives. Many variations of the central chain lead to compounds of reduced activity, the outstanding exceptions being a number of but‐2‐ene derivatives, which retain full activity.

THE SCHISTOSOMICIDAL AND TOXIC EFFECTS OF SOME αω‐DI(p‐AMINOPHENOXY)ALKANES AND RELATED MONOAMINES

“…This field was covered thoroughly by Raison and Standen (1955) and Gorvin et al (1957). Our results agree very well with theirs with the single exception of the isopropyl derivative, which Raison and Standen (1955) found to be active.…”

“…Branched chains (Table II) had a deleterious effect, as Gorvin et al (1957) also found, but compounds with a double bond in the chain were as active as those with a saturated chain. It is doubtful if the apparent difference in activity between the cis and trans isomers was significant.…”

“…It is doubtful if the apparent difference in activity between the cis and trans isomers was significant. The two compounds with a triple bond which we examined were completely inactive although Gorvin et al (1957) found activity in some acetylenic compounds, the activity increasing with the distance between one oxygen atom and the triple bond. The replacement of the central chain with a carbocyclic ring was also dystherapeutic, the activity decreasing from cyclohexene through cyclohexane to benzene.…”

“…Consequently two groups of workers have quite independently set out from virtually the same chemical starting point and followed paths which have sometimes crossed but more often diverged. Inevitably the two research studies overlap to some extent, especially in the early phases (Raison and Standen, 1955;Caldwell and Standen, 1956;Standen and Walls, 1956;Gorvin, Raison, Solomon, Standen and Walls, 1957).…”

The Antischistosomal and Retinotoxic Effects of Some Nuclear Substituted Aminophenoxyalkanes

“…Effect of N-substitution (Table 9) The results given here demonstrate that N-substituted compounds were active although they were sometimes less so than the corresponding primary amines, as found by Raison & Standen (1955); Gorvin, Raison, Solomon, Standen & Walls (1957) and Collins et al (1958Collins et al ( , 1959.…”