72801-61-7Relevant articles and documents
Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study
Labib, Madlen B.,Sharkawi, Souty M.Z.,El-Daly, Mahmoud
, p. 70 - 80 (2018)
A group of novel isoindoline hybrids incorporating oxime, hydrazone, pyrazole, chalcone or aminosulfonyl pharmacophores (9–14) was designed and characterized by spectral data and elemental analyses results. All newly synthesized compounds were evaluated as COX-2 inhibitors, anti-inflammatory and analgesic agents. Six hybrid derivatives (10b, 10c, 11a, 11d, 13, 14) were moderate COX-2 inhibitors (IC50 = 0.11–0.18 μM) close to standard celecoxib (IC50 = 0.09 μM). The most active compounds showed outstanding in vivo anti-inflammatory activity (% edema inhibition = 41.7–50, 1 h; 40.7–67.4, 3 h; 20–46.7, 6 h) better than reference drug diclofenac (% edema inhibition = 29.2, 1 h; 22.2, 3 h; 20, 6 h). Most compounds showed significant peripheral and/or central analgesic activity. The moderate selective COX-2 inhibitor; dimethoxychalcone 11d (SI = 103) displayed excellent anti-inflammatory activity (% edema inhibition = 45.8–59.3) and increased thermal pain threshold (50–92.85%) comparable to piroxicam (75%). Molecular docking studies have been established.
High-triplet-level phthalimide based acceptors for exciplexes with multicolor emission
Chapran, Marian,Lytvyn, Roman,Begel, Corentin,Wiosna-Salyga, Gabriela,Ulanski, Jacek,Vasylieva, Marharyta,Volyniuk, Dmytro,Data, Przemyslaw,Grazulevicius, Juozas Vidas
, p. 872 - 882 (2018/11/24)
To provide high exciton utilization in organic light emitting diodes, phthalimide derivatives were designed and synthesized as exciplex-forming materials. Due to high triplet levels (2.92–3.11 eV) and ionization potentials (7.18–7.29 eV), the developed phthalimide derivatives were found to be not only appropriate accepting materials for the formation of different color exciplexes but also as bifunctional materials with a satisfactory hole and exciton-blocking abilities. Solid-state blends of the synthesized phthalimides as acceptors and a carbazole containing donors showed exciplex emission. Bimolecular blends exhibited multicolor exciplex emission which covered a visible spectrum from sky-blue to red colors, depending on the donor used. However, the photoluminescence quantum efficiencies of the studied exciplex-forming systems were found to be sensitive to the molecular design of the phthalimides. Acceptor with para-substituted phthalimide showed better exciplex-forming properties in comparison to other compounds. Exciplex-forming blend of (2-(4-benzoylphenyl)isoindoline-1,3-dione) as an acceptor and 1,3-di(9H-carbazol-9-yl)benzene (mCP) as a donor showed the most efficient sky-blue emission with small singlet-triplet splitting (0.06 ± 0.03eV). Such exciplex-forming molecular mixture was implemented as the light-emitting material in the sky-blue organic light emitting diodes which showed the brightness of 2500 cd m?2 and maximum external quantum efficiency of 2.9% due to the employment of both singlet and triplet excitons.
Hypolipidemic Activity of Phthalimide Derivatives. 2. N-Phenylphthalimide and Derivatives
Chapman, James M.,Voorstad, P. Josee,Cocolas, George H.,Hall, Iris H.
, p. 237 - 243 (2007/10/02)
A series of substituted N-phenylphthalimide derivatives was synthesized and examined for their ability to lower serum cholesterol and triglyceride levels in mice at 20 (mg/kg)/day, ip.Of the newly synthesized compounds, the most potent compound, o-(N-phthalimido)acetophenone, lowered serum cholesterol 57percent after 16 days and lowered serum triglyceride levels 44percent after 14 days. o-(N-Phthalimido)acetophenone was observed to be active in both normogenic (normal blood lipids levels) and hyperlipidemic mice and normogenic rats.In the latter, the reduction of serum lipids was reversible.The mode of action of this compound appeared to be multiple, including blockage of the de novo synthesis of lipids and acceleration of the excretion of lipids.The lipoprotein fractions of rat blood were reduced significantly in cholesterol, triglyceride, and neutral lipid content after 14 days treatment with o-(N-phthalimido)acetophenone.
