New Antiparasitic Agents

Abstract

Some acridine compounds referred to as 9-imino, 9-oxo and 9-thio derivatives were screened for activity against Trypanosoma cruzi in vitro. The results are discussed here with reference to the structure of the compounds tested. Attempts to elucidate the mode of action of active acridines are also included. The most active compounds that were tested were 9-thioacridanones and 9-thio-1,2,3,4-tetrahydroacrida-nones. Added to this, the dialkylaminoalkylthio group seems to be the most convenient molecular moiety for trypanocidal activity in the 9-substituted acridine series.

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

“…Acridine derivatives are currently delivered to animals as antihelminthics and antiprotozoals [2]. 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].…”

Preparation of some new N-substituted 9,10-dihydroacridine derivatives

“…In conclusion, It must be emphasized that, despite the fact that the methods used are very convenient for preparing 9,10-dihydroacridines, the latter are not useful compounds. CuHnNO (209.25) 8.5 (m, 2 H), 7.65 (m, 2 H), 7.25 (m, 4 H), 3.8 (s, 3 H) 2b ch2-ch2-ch3 80 130 (9) C16H16NO (237.30) 8.5 (m, 2 H), 7.55 (m, 2 H), 7.2 (m, 4 ), 4.1 (t, 2 ), 1.8 (m, 2 ), 1.05 (t, C19H22N20 (294.40) 8.6 (m, 2 H), 7.8 (m, 2 H), 7.6 (m, 2 H), 7.3 (m, 2 H), 4.5 (t, 2 H), 2.9 (t, 2 H), 2.75 (q, 4 ), C2"H22N20 (306.41) 8.5 (m, 2 H), 7.75 (m, 2 H), 7.5 (m, 2 H), 7.25 (m, 2 H),…”

“…7.1 (m, 4 H), 6.9 (m, 2 H), 6.65 (m, 2 ), 7.5 (m, 4 H), 6.9 (m, 4 ), 4.0 (m, 1 H), 3.8 (s, 2 H), 3.65 (m, 1 H), 2.2 (m, 9 ), 0.9 (d, 3 H) 3f c7h14n 90 68 CaoH^Nj (292.43)…”

“…7.2 (m, 4 ), 7.0 (m, 4 ), 4.15 (t, 2 ), 4.0 (s, 2 H), 2.75 (t, 2 H), 2.55 (m, 4 ), 1.7 (m, 4 ), 1.5 (m, 2 H) 3g c6h12n b C19H22N2 (278.40) 7.1 (m, 4 H), 6.9 (m, 4 ), 4.1 (t, 2 ), 4.0 (s, 2 H), 2.95 (t, 2 H), 2.7 (m, 4 ), 1.9 (m, 4 H) 3h c6h12no 86 105 C19H22N20 (294.40) 7.15 (m, 4 H), 6.9 (m, 4 ), 4.1 (t, 2 H), 3.95 (s, 2 H), Indeed, they lead back to the 9-oxo homologues within a few weeks even if they are bottled In brown flasks, safe from air. This has been proved by TLC.…”