Antiamebic Activity of New Acridinic Derivatives against <i>Naegleria </i>and <i>Acanthamoeba </i>Species in vitro

Abstract

In vitro antiamebic activity of selected acridine derivatives has been investigated against Naegleria and Acanthamoeba species. The most active compounds belong to the 9-thioacridanone and the 1,2,3,4-tetrahydro-9-thioacridanone series. In addition, some structure-activity relationships are proposed.

New Antiamebic Acridines

“…A number of the compounds synthe sized were submitted for testing for antiparasitic activity against the Umax ameba Naegleria fowleri which is the causative agent of an ordinary fatal meningoence phalitis [9]. The results are summarized in table III.…”

“…Some of these compounds have already been evaluated for antiamebic ac tivity against Naegleria fowleri. Results were presented in part I [9].…”

New Antiparasitic Agents

“…This work (Part I [5], II [6] and III) was supported in part by a grant from the Conseil Régional PACA (subv. 85/4568 PLA).…”

“…Yet, this activity has been pointed out in the case of various 9-substi tuted acridinic compounds such as 9-aminoacridines [1,2] including mepacrine [3] or ledakrin [1], 9-azidoacridines [1], 9-phenylacridines as well as 9-acridanones [4], On the other hand, antiprotozoal activ ity is commonly examined by using strains of Trypanosoma brucei [ 1 ], so that there are almost no investigations concerning Try panosoma cruzi in the series under discus sion, despite the acute need for an efficient therapy for Chagas' disease. With this in mind, a set of new derivatives showing antiamebic activity in vitro [5,6] was screened for activity against T. cruzi in vitro. The prepared acridines belong to the following series: 9-iminoacridine, 1, 9-acridanone, 2, 9-thioacridanone, 3, and 9-thialkylacridine, 4, as well as 1,2,3,4-tetrahydro-9-acridanone, 5, and 1,2,3,4-tetrahydro-9-thioacridanone, 6.…”

Inhibition of Cryptosporidium parvum in vitro by 9-(Alkylthio)acridine Derivatives

“…Moreover, acridine dyes such as mepacrine, are probably drugs of choice for giardiasis in human and different acridine derivatives have shown in vitro to be effective against Trypanosoma cruzi [3,6], Leishmania spp. [6,7] and amphizoic amoebae [6,8]. Thus, we were interested in studying on MDCK cells the in vitro action of newly synthesized 9-(alkylthio)acridines in the first stages of Cryptosporidium parvum development.…”