AROMATIC GUANYL HYDRAZONES - SYNTHESIS, STRUCTURAL STUDIES AND IN-VITRO ACTIVITY AGAINST TRYPANOSOMA-CRUZI

Citation
Jc. Messeder et al., AROMATIC GUANYL HYDRAZONES - SYNTHESIS, STRUCTURAL STUDIES AND IN-VITRO ACTIVITY AGAINST TRYPANOSOMA-CRUZI, Bioorganic & medicinal chemistry letters, 5(24), 1995, pp. 3079-3084
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
ISSN journal
0960894X
Volume
5
Issue
24
Year of publication
1995
Pages
3079 - 3084
Database
ISI
SICI code
0960-894X(1995)5:24<3079:AGH-SS>2.0.ZU;2-L
Abstract
A series of 22 aromatic guanyl hydrazones, prepared by condensation of several aldehydes with aminoguanidine hydrochloride, were fully chara cterized by NMR techniques and tested in vitro against the trypomastig ote form of Trypanosoma cruzi, the causative agent of Chagas disease. Most of the compounds, especially those without hydrogen bonding group s and possessing ortho-substitution, were significantly more active th an crystal violet (ID50 536 mu M). The most active compound has an ID5 0 value of 17 mu M (25 times more potent than gentian violet).