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

2,1,3-Benzothiadiazine derivatives: synthesis and screening versus PDE4 enzyme / Tait, Annalisa; Luppi, Amedeo; Avallone, Rossella; Baraldi, Mario. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 60:8(2005), pp. 653-663. [10.1016/j.farmac.2005.05.009]

2,1,3-Benzothiadiazine derivatives: synthesis and screening versus PDE4 enzyme

TAIT, Annalisa;AVALLONE, Rossella;BARALDI, Mario
2005

Abstract

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
2005
60
8
653
663
2,1,3-Benzothiadiazine derivatives: synthesis and screening versus PDE4 enzyme / Tait, Annalisa; Luppi, Amedeo; Avallone, Rossella; Baraldi, Mario. - In: IL FARMACO. - ISSN 0014-827X. - STAMPA. - 60:8(2005), pp. 653-663. [10.1016/j.farmac.2005.05.009]
Tait, Annalisa; Luppi, Amedeo; Avallone, Rossella; Baraldi, Mario
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11380/309605
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