Computational design, synthesis and biological evaluation of PDE5 inhibitors based on N2, N4-diaminoquinazoline and N2, N6-diaminopurine scaffolds
T Somnarin, N Pobsuk, R Chantakul, T Panklai… - Bioorganic & Medicinal …, 2022 - Elsevier
We report the synthesis, and characterization of twenty-nine new inhibitors of PDE5.
Structure-based design was employed to modify to our previously reported 2, 4 …
Structure-based design was employed to modify to our previously reported 2, 4 …
New imidazolone derivatives comprising a benzoate or sulfonamide moiety as anti-inflammatory and antibacterial inhibitors: Design, synthesis, selective COX-2 …
NH Metwally, MS Mohamed - Bioorganic Chemistry, 2020 - Elsevier
Abstract New imidazol-5-one derivatives 12a, b and 12e, f, 14a, b and 16a, b were
synthesized and screened for their in vivo anti-inflammatory activity using a standard acute …
synthesized and screened for their in vivo anti-inflammatory activity using a standard acute …
Design, Synthesis, and Structure− Activity Relationship, Molecular Modeling, and NMR Studies of a Series of Phenyl Alkyl Ketones as Highly Potent and Selective …
Phosphodiesterase 4 catalyzes the hydrolysis of cyclic AMP and is a target for the
development of anti-inflammatory agents. We have designed and synthesized a series of …
development of anti-inflammatory agents. We have designed and synthesized a series of …
Analogue-based design, synthesis and molecular docking analysis of 2, 3-diaryl quinazolinones as non-ulcerogenic anti-inflammatory agents
E Manivannan, SC Chaturvedi - Bioorganic & medicinal chemistry, 2011 - Elsevier
In our effort to identify potent gastric sparing anti-inflammatory agents, a series of methyl
sulfanyl/methyl sulfonyl substituted 2, 3-diaryl quinazolinones were designed by analogue …
sulfanyl/methyl sulfonyl substituted 2, 3-diaryl quinazolinones were designed by analogue …
Synthesis, biological evaluation and docking studies of novel benzopyranone congeners for their expected activity as anti-inflammatory, analgesic and antipyretic …
AAM Eissa, NAH Farag, GAH Soliman - Bioorganic & Medicinal Chemistry, 2009 - Elsevier
8-Acetyl-7-hydroxy-4-phenyl-2H-benzopyran-2-one as starting material a number of 8-
substituted derivatives (ie, hydrazones 2a, b, imine 2c, chalcones 3, pyrazoles 4, 3-cyano-2 …
substituted derivatives (ie, hydrazones 2a, b, imine 2c, chalcones 3, pyrazoles 4, 3-cyano-2 …
Synthesis of novel naphthalimide tethered 1, 2, 3-triazoles: In vitro biological evaluation and docking study of anti-inflammatory inhibitors
R Begam, A Shajahan, B Shefin, V Murugan - Journal of Molecular …, 2022 - Elsevier
In this research work, a novel heterocyclic naphthalimide tethered 1, 2, 3-triazoles was
synthesized by the approach of click chemistry. An entire compound's chemical structure …
synthesized by the approach of click chemistry. An entire compound's chemical structure …
Synthesis and bioactivity of 3, 5-dimethylpyrazole derivatives as potential PDE4 inhibitors
DK Hu, DS Zhao, M He, HW Jin, YM Tang… - Bioorganic & medicinal …, 2018 - Elsevier
Abstract A series of 3, 5-dimethylpyrazole derivatives containing 5-phenyl-2-furan moiety
were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. Bioassay …
were designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. Bioassay …
Synthesis and bioactivity of phenyl substituted furan and oxazole carboxylic acid derivatives as potential PDE4 inhibitors
Y Lin, W Ahmed, M He, X Xiang, R Tang… - European Journal of …, 2020 - Elsevier
In this present study, a series of 5-phenyl-2-furan and 4-phenyl-2-oxazole derivatives were
designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results …
designed and synthesized as phosphodiesterase type 4 (PDE4) inhibitors. In vitro results …
Structure-based optimization of Toddacoumalone as highly potent and selective PDE4 inhibitors with anti-inflammatory effects
F Zhou, Y Huang, L Liu, Z Song, KQ Hou, Y Yang… - Biochemical …, 2022 - Elsevier
Abstract Phosphodiesterase-4 (PDE4) is an important drug target for inflammatory diseases.
Previously, we identified a series of novel PDE4 inhibitors derived from the natural …
Previously, we identified a series of novel PDE4 inhibitors derived from the natural …
Synthesis, molecular docking and biological evaluation of some newer 2-substituted-4-(benzo [d][1, 3] dioxol-5-yl)-6-phenylpyridazin-3 (2H)-ones as potential anti …
A new series of 2-substituted-4-(benzo [d][1, 3] dioxol-5-yl)-6-phenylpyridazin-3 (2H)-one
derivatives has been synthesized and studied. The in vivo anti-inflammatory and analgesic …
derivatives has been synthesized and studied. The in vivo anti-inflammatory and analgesic …