Some Structure-Activity Relationships Among Aziridinyl Antifertility Agents in Screw-Worm Flies12

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Abstract
Candidate chemosterilants with 1, 2, or more molecular aziridinyl groups were screened topically and orally against adult screw-worm flies, Cochliomyia homitlivorax (Coquerel). Sexual sterility of the flies and number of unsubstituted functional groups were largely unrelated. However, more compounds with 3 or more substituted groups (56%) were active topically than with fewer substituted groups (14%), but they were equal to unsubstituted polyfunctional compounds (53%). Otherwise, about twice as many compounds with unsubstituted aziridinyl carbon atoms were effective as those that were substituted. Toxicity was independent of number of functional groups, irrespective of substitution. In general, more compounds were potent chemosterilants (90%) and nontoxic (38%) when administered multiple orally than topically (44% and 20%, respectively). Sterility, after oral administration, resulted from cumulative action of all monofunctional and half of all other aziridinyl compounds.

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