In silico and in vitro ADME-Tox analysis and in vivo pharmacokinetic study of representative pan-PDE inhibitors from the group of 7, 8-disubstituted derivatives of 1, 3 …

K Wójcik-Pszczoła, M Szafarz, K Pociecha… - Toxicology and Applied …, 2022 - Elsevier
Phosphodiesterase (PDE) inhibitors represent a wide class of chemically different
compounds that have been extensively studied in recent years. Their anti-inflammatory and …

[HTML][HTML] Synthesis and in vitro evaluation of anti-inflammatory, antioxidant, and anti-fibrotic effects of new 8-aminopurine-2, 6-dione-based phosphodiesterase …

K Wójcik-Pszczoła, A Jankowska, M Ślusarczyk… - Bioorganic …, 2021 - Elsevier
Phosphodiesterase (PDE) inhibitors are currently an extensively studied group of
compounds that can bring many benefits in the treatment of various inflammatory and fibrotic …

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

A Tait, A Luppi, A Hatzelmann, P Fossa… - Bioorganic & medicinal …, 2005 - Elsevier
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 …

Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases

E Armani, G Amari, A Rizzi, RD Fanti… - Journal of Medicinal …, 2014 - ACS Publications
The first steps in the selection process of a new anti-inflammatory drug for the inhaled
treatment of asthma and chronic obstructive pulmonary disease are herein described. A …

Discovery of novel purine nucleoside derivatives as phosphodiesterase 2 (PDE2) inhibitors: Structure-based virtual screening, optimization and biological evaluation

X Qiu, Y Huang, D Wu, F Mao, J Zhu, W Yan… - Bioorganic & Medicinal …, 2018 - Elsevier
Abstract Phosphodiesterase 2 (PDE2) has received much attention for the potential
treatment of the central nervous system (CNS) disorders and pulmonary hypertension …

Novel butanehydrazide derivatives of purine-2, 6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: design, synthesis and biological evaluation

G Chłoń-Rzepa, A Jankowska, M Ślusarczyk… - European journal of …, 2018 - Elsevier
A novel butanehydrazide derivatives of purine-2, 6-dione designed using a ligand-based
approach were synthesized and their in vitro activity against both PDE4B and PDE7A …

Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: design, synthesis, and structure-activity relationship study of …

ZZ Zhou, BC Ge, QP Zhong, C Huang, YF Cheng… - European Journal of …, 2016 - Elsevier
In this study, catecholamides (7a–l) bearing different aromatic rings (such as pyridine-2-yl,
pyridine-3-yl, phenyl, and 2-chlorophenyl groups) were synthesized as potent …

Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors

YS Li, XY Liu, DS Zhao, YX Liao, LH Zhang… - Bioorganic & medicinal …, 2018 - Elsevier
Tetrahydroquinoline and tetrahydroisoquinoline derivatives containing 2-phenyl-5-furan
moiety were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. The …

[HTML][HTML] Synthesis, pharmacological profile and docking studies of new sulfonamides designed as phosphodiesterase-4 inhibitors

IKC Nunes, ET de Souza, SVS Cardozo, VF Carvalho… - PLoS …, 2016 - journals.plos.org
Prior investigations showed that increased levels of cyclic AMP down-regulate lung
inflammatory changes, stimulating the interest in phosphodiesterase (PDE) 4 as therapeutic …

Structure-based design and structure-activity relationships of 1, 2, 3, 4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors

Y Liao, Y Guo, S Li, L Wang, Y Tang, T Li… - Bioorganic & Medicinal …, 2018 - Elsevier
This paper describes our medicinal chemistry efforts on 7-(cyclopentyloxy)-6-methoxy1, 2, 3,
4-tetrahydroisoquinoline scaffold: design, synthesis and biological evaluation using …