Elsevier
Bioorganic and Medicinal Chemistry
,  том 13 ,  издание 4 ,  страницы 1393-1402

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

Тип публикации: Journal Article
Дата публикации: 2005-02-01
Elsevier
scimago Q2
wos Q1
БС1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3
ISSN: 09680896, 14643391
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
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 antioxidant compound 13 was found active and selective at micromolar level versus PDE4. 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 N1 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.
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Tait A. et al. Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors // Bioorganic and Medicinal Chemistry. 2005. Vol. 13. No. 4. pp. 1393-1402.
ГОСТ со всеми авторами (до 50) Скопировать
Tait A., Luppi A., Hatzelmann A., Fossa P., Mosti L. Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors // Bioorganic and Medicinal Chemistry. 2005. Vol. 13. No. 4. pp. 1393-1402.
RIS |
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TY - JOUR
DO - 10.1016/j.bmc.2004.10.055
UR - https://doi.org/10.1016/j.bmc.2004.10.055
TI - Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors
T2 - Bioorganic and Medicinal Chemistry
AU - Tait, A.
AU - Luppi, Amedeo
AU - Hatzelmann, Armin
AU - Fossa, Paola
AU - Mosti, Luisa
PY - 2005
DA - 2005/02/01
PB - Elsevier
SP - 1393-1402
IS - 4
VL - 13
PMID - 15670947
SN - 0968-0896
SN - 1464-3391
ER -
BibTex |
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@article{2005_Tait,
author = {A. Tait and Amedeo Luppi and Armin Hatzelmann and Paola Fossa and Luisa Mosti},
title = {Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors},
journal = {Bioorganic and Medicinal Chemistry},
year = {2005},
volume = {13},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.bmc.2004.10.055},
number = {4},
pages = {1393--1402},
doi = {10.1016/j.bmc.2004.10.055}
}
MLA
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Tait, A., et al. “Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors.” Bioorganic and Medicinal Chemistry, vol. 13, no. 4, Feb. 2005, pp. 1393-1402. https://doi.org/10.1016/j.bmc.2004.10.055.