Synthesis and antichagasic properties of new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides and related compounds

Citation
R. Di Maio et al., Synthesis and antichagasic properties of new 1,2,6-thiadiazin-3,5-dione 1,1-dioxides and related compounds, ARZNEI-FOR, 49(9), 1999, pp. 759-763
Citations number
14
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
ISSN journal
00044172 → ACNP
Volume
49
Issue
9
Year of publication
1999
Pages
759 - 763
Database
ISI
SICI code
0004-4172(199909)49:9<759:SAAPON>2.0.ZU;2-#
Abstract
In a search for antichagasic drugs, 14 new 4-(nitroarylidene)-1,2,6-thiadia zin-3,5-dione 1,1-dioxide derivatives were synthesized and tested in vitro against the epimastigote form of Trypanosoma cruzi and some of them showed important antiprotozoan activity. Attempts to synthesize new 4-(nitroarylid ene)-3,5-diamino-1,2,6-thiadiazine 1,1-dioxides were unsuccessful. The anti chagasic properties of nitroarylidene-malononitrile and nitroarylidene-cyan oacetamide derivatives, thus obtained, were also tested. The cytotoxic prop erties against Vero cells of compounds which showed remarkable in vitro ant ichagasic activity were evaluated. All compounds tested exhibited high toxi city percentages at 100 mu g/ml. However, compound 3c showed in vitro antic hagasic and cytotoxic properties such as nifurtimox at the dose of 10 mu g/ ml.