255911-25-2Relevant academic research and scientific papers
Chlorophenylmethyl benzothiadiazine dioxides derivatives: Potent human cytomegalovirus inhibitors
Martinez, Ana,Gil, Carmen,Perez, Concepcion,Castro, Ana,Prieto, Columbiana,Otero, Joaquin
, p. 3133 - 3136 (1999)
Modifications of our previously reported lead compounds, acyclonucleosides derived from 2,1,3-benzothiadiazine dioxides, in the search for inhibitors of human cytomegalovirus (HCMV), lead us to identify the chlorophenylmethyl benzothiadiazine dioxides derivatives as potent HCMV inhibitors. The synthesis and antiviral data of this second-generation of benzothiadiazine dioxide compounds are reported.
Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: First phosphodiesterase 7 inhibitors
Martínez, Ana,Castro, Ana,Gil, Carmen,Miralpeix, Montserrat,Segarra, Victor,Doménech, Teresa,Beleta, Jorge,Palacios, Jose M.,Ryder, Hamish,Miró, Xavier,Bonet, Carles,Casacuberta, Josep M.,Azorín, Ferran,Pi?a, Benjamí,Puigdoménech, Pere
, p. 683 - 689 (2007/10/03)
The synthesis of a new family of benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]-thiadiazine 2,2-dioxides was achieved. The biological data revealed the first heterocyclic family of compounds with PDE 7 inhibitory properties appearing to be a new objective for the treatment of T-cell- dependent disorders. The IC50 values or percent inhibition values of the compounds against PDE 7 were calculated by testing them against human recombinant PDE 7 expressed in S. cerevisiae. In this expression system the only cyclic nucleotide hydrolyzing activity present in cell extracts corresponded to human PDE 7. Isoenzyme selectivity PDE 7 versus PDE 4 and PDE 3 was also measured. Considering simultaneously inhibition of the three different isoenzymes, monobenzyl derivatives 15 and 23 showed interesting PDE 7 potency (around 10 μM); although not statistically significant, a trend toward selectivity with respect to PDE 3 and PDE 4 was obtained. Benzothiadiazine 16, although less potent at PDE 7 (IC50 = 25 μM), also showed a trend of selectivity toward PDE 3 and PDE 4. These compounds are considered the best leads for further optimization.
