Synthesis and Antiprotozoal Evaluation of New N4-(Benzyl)spermidyl-linked bis(1,3,5-thiadiazinane-2-thiones)

• Published in: Archiv der Pharmazie (Weinheim) Vol. 341; no. 11; pp. 708 - 713
• Main Authors: Coro, Julieta, Little, Susan, Yardley, Vanessa, Suárez, Margarita, Rodríguez, Hortensia, Martín, Nazario, Perez-Pineiro, Rolando
• Format: Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01-11-2008; WILEY‐VCH Verlag
• Subjects: 1,3,5‐Thiadiazinane‐2‐thione; 5-Thiadiazinane-2-thione; Animals; Antiprotozoal Agents - chemical synthesis; Antiprotozoal Agents - pharmacology; Drug Evaluation, Preclinical; Leishmania donovani; Leishmania donovani - drug effects; Protozoocidal activity; Spermidine; Spermidine - chemistry; Structure-Activity Relationship; Thiones - chemical synthesis; Thiones - pharmacology; Trypanosoma cruzi; Trypanosoma cruzi - drug effects
• ISSN: 0365-6233; 1521-4184
• DOI: 10.1002/ardp.200800011

The synthesis and in‐vitro antiprotozoal evaluation of novel N4‐(benzyl)spermidyl‐linked bis(1,3,5‐thiadiazinane‐2‐thione) (bis‐THTT) derivatives from N4‐(benzyl)spermidine is disclosed. Several of the new bis‐THTT have in‐vitro activities against L. donovani and T. cruzi that are comparable or superior to those of currently employed protozoocidal agents.