IN-VITRO ANTIFILARIAL EVALUATION OF PHENOXYCYCLOHEXANE DERIVATIVES

Numerous potential inhibitors of the phosphoenolpyruvate-carboxylase found in Molinema dessetae were synthesized and evaluated as inhibitors of the purified enzyme and as killers, in vitro, of M. dessetae adult females and infective larvae. Phosphoenolpyruvate analogs (or derivatives) appeared disappointing whereas phenoxycyclohexane derivatives inhibited the enzyme in a non-competitive manner and killed the parasites. The compounds P2281 and P2285, for example, had K(i) values of 122 and 93 μM, respectively. In vivo tests of the most effective phenoxycyclohexanes will now be carried out to check their potential as antifilarial drugs.