Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors

Tait, Annalisa; Luppi, A.; Hatzelmann, A.; Fossa, P.; Mosti, L.

A series of 2,1,3- and 1,2,4-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity versus enzymatic isoforms PDE3, PDE4 and PDE7. The compounds characterized by the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at NI position of 2,1,3-benzothiadiazine core (8, 13, 18), were found active and selective at micromolar level versus PDE4 and could be studied as new leads for the treatment of asthma and COPD (Chronic Obstructive Pulmonary Disease). The antioxidant activity evaluation on the same compounds highlighted 13 as the most significative. Molecular modelling studies gave further support to biological results and suggested targeted modifications so as to improve their potency. (C)2004 Elsevier Ltd. All rights reserved.

Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors / Tait, Annalisa; A., Luppi; A., Hatzelmann; P., Fossa; L., Mosti. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 13(2005), pp. 1393-1402.

Data di pubblicazione:	2005
Titolo:	Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors
Autore/i:	Tait, Annalisa; A., Luppi; A., Hatzelmann; P., Fossa; L., Mosti
Autore/i UNIMORE:	TAIT, Annalisa A. Luppi A. Hatzelmann P. Fossa L. Mosti mostra contributor esterni nascondi contributor esterni
Rivista:	BIOORGANIC & MEDICINAL CHEMISTRY
Volume:	13
Pagina iniziale:	1393
Pagina finale:	1402
Codice identificativo ISI:	WOS:000226967900046
Codice identificativo Scopus:	2-s2.0-12844253180
Codice identificativo Pubmed:	15670947
Citazione:	Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors / Tait, Annalisa; A., Luppi; A., Hatzelmann; P., Fossa; L., Mosti. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 13(2005), pp. 1393-1402.
Tipologia	Articolo su rivista

File in questo prodotto:

File	Descrizione	Tipologia
Biorganic 2005.pdf		Post-print dell'autore (bozza post referaggio)	Administrator Richiedi una copia

Utilizza questo identificativo per citare o creare un link a questo documento:
http://hdl.handle.net/11380/305647

Citazioni

I documenti presenti in Iris Unimore sono rilasciati con licenza Creative Commons Attribuzione - Non commerciale - Non opere derivate 3.0 Italia, salvo diversa indicazione.
In caso di violazione di copyright, contattare Supporto Iris