Abstract:
:Six lycorine derivatives were prepared, characterized, and evaluated for their in vitro anti-Trichomonas vaginalis activity. Compounds bearing an acetyl (2), lauroyl (3), benzoyl (4 and 5), and p-nitrobenzoyl (6 and 7) groups were synthesized. The best activity was achieved with lycorine esterified at C-2 position with lauroyl group. Preliminary structure-activity relationship points that unprotected OH group at C-1 and C-2 is not necessary to the antiparasitic activity, and none of the derivative was less active than lycorine. The lycorine structural requisites required to kill this amitochondriate cell seem to be different in comparison with the derivatives most active against other parasites and tumor cell lines, both mitochondriated cells. This result is an important contribution with our ongoing studies regarding the mechanism of action of the Amaryllidaceae alkaloids on T. vaginalis cell death opening a new perspective to optimize this innovative pharmacological potential.
journal_name
Chem Biol Drug Desjournal_title
Chemical biology & drug designauthors
Giordani RB,Junior CO,de Andrade JP,Bastida J,Zuanazzi JA,Tasca T,de Almeida MVdoi
10.1111/j.1747-0285.2012.01333.xsubject
Has Abstractpub_date
2012-07-01 00:00:00pages
129-33issue
1eissn
1747-0277issn
1747-0285journal_volume
80pub_type
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