810661-20-2Relevant academic research and scientific papers
2,1,3-Benzothiadiazine derivatives: Synthesis and screening versus PDE4 enzyme
Tait, Annalisa,Luppi, Amedeo,Avallone, Rossella,Baraldi, Mario
, p. 653 - 663 (2007/10/03)
A series of N-1,3 disubstituted 2,1,3-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity versus enzymatic isoform PDE4 extracted from U937 cell line. Some of the tested compounds showed a high PDE4 inhibitory activity at 100:μM and the IC50 value of the most interesting terms were evaluated. The structure-activity relationships of these compounds showed that the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at N-1 position is important to obtain activity at micromolar level as previously reported. For the same compounds the antioxidant activity were evaluated highlighting 14 as the most significative one. The introduction of other bulky substituents in N-1 position is detrimental.
Synthesis and antiviral activity of new benzothiadiazine dioxide derivatives
Tait, Annalisa,Luppi, Amedeo,Cermelli, Claudio
, p. 747 - 753 (2007/10/03)
A series of 2,1,3- and 1,2,4-benzothiadiazine derivatives were synthesized by alkylation via Mitsunobu reaction and evaluated for their antiviral activity against ADV, HHV-6, Cox-B5 and H-CMV. Most of them were active at micromolar level against one or more viral strains. All the molecules studied are poorly cytotoxic (maximum non toxic concentrations were >25μM), except one compound that presents a higher cytotoxicity (maximum non toxic concentration was 6 μM).
