Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds

• Published in: Bioorganic & medicinal chemistry letters 2001-10, Vol.11 (20), p.2755-2757
• Main Authors: Olmo, Esther del, Armas, Marlon Garcı́a, López-Pérez, Jose Luis, Ruiz, Grace, Vargas, Fernando, Giménez, Alberto, Deharo, Eric, Feliciano, Arturo San
• Format: Article
• Language: English
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiparasitic agents; Biological and medical sciences; Medical sciences; Parasitic Sensitivity Tests; Pharmacology. Drug treatments; Stilbenes - chemical synthesis; Stilbenes - chemistry; Stilbenes - pharmacology; Structure-Activity Relationship; Trypanocidal Agents - chemical synthesis; Trypanocidal Agents - chemistry; Trypanocidal Agents - pharmacology; Trypanosoma cruzi - drug effects
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/S0960-894X(01)00562-5

We report the anti-Chagasic activity of the natural dihydrostilbenoid isonotholaenic acid and several simple derivatives, as well as that of some representative compounds of related synthetic series, with basic structures of benzalphthalides, dihydrostilbamides, isoindoles, phthalazin-1-ones, imidazo[2,1 -a]isoindoles and pyrimido[2,1 -a]isoindoles. The evaluation was performed in vitro on cultures of epimastigote and trypomastigote forms of Trypanosoma cruzi. Some of the tested compounds resulted to be as potent as benznidazole (epimastigotes), and others were shown to be more active than gentian violet (trypomastigotes), used as reference drugs. The natural dihydrostilbene isonotholaenic acid, semi-synthetic derivatives and total synthetic analogues, displaying benzalphthalide, dihydrostilbamide, phthalazinone, and imidazo/pyrimido-isoindole structures, have been obtained and tested on anti-trypanosome assays.