Isoindoline-1,3-dione derivatives constitute an important group of medicinal substances. In this study, nine new 1H-isoindole-1,3(2H)-dione and five potential pharmacophores were obtained in good yield (47.24–92.91%). The structure the imides was confirmed by methods elemental spectral analysis: FT–IR, H NMR, MS. Based on results ESI–MS probable path molecules decay hypothetical resulting pseudo-molecular ions have been proposed. physicochemical properties phthalimides determined basis...

Many publications in databases deal with the interactions of new drugs albumin. However, it is not only albumin that responsible for binding pharmaceutical molecules to proteins human body. There are many more plasma important study ADME pathway. Therefore, this study, we have shown results between albumin, orosomucoid, and gamma globulins non-toxic anti-inflammatory phthalimide analogs, which due promising obtained results, may be potential candidates group analgesic drugs. Using...

Inhibition of cyclooxygenase is the way therapeutic activities for anti-inflammatory pharmaceuticals. Serum albumins are major soluble protein able to bind and transport a variety exogenous endogenous ligands, including hydrophobic In this study, novel N-substituted 1H-pyrrolo[3–c]pyridine-1,3(2H)-diones derivatives were synthesized biologically evaluated their inhibitory activity against cyclooxygenases interactions with BSA. vitro, COX-1 COX-2 inhibition assays performed. Interaction BSA...

The derivatives of isoindoline-1,3-dione are interesting due to their biological activities, such as anti-inflammatory and antibacterial effects. Several series have been designed evaluated for Alzheimer's therapy candidates. They showed promising activity. In this work, six new were first tested in silico studies inhibitory ability against acetylcholinesterase (AChE) butyrylcholinesterase (BuChE) enzymes. Molecular docking molecular dynamic simulation applied. Next, these compounds...

One of the groups organic compounds with potential use in medicine and pharmacy is phthalimide derivatives. They are characterized by a wide range properties such as antibacterial, antifungal, anti-inflammatory. In this study, we focused on research four derivatives proven non-toxicity, which cyclooxygenase inhibitors. With molecular docking study spectroscopic methods, fluorescence, circular dichroism, FT-IR spectroscopies, analyzed way tested interact plasma proteins. Among many proteins...

Abstract The stress and accelerated tests as well photostability analysis in solutions the solid phase of three selected derivatives pyrrolo[3,4-c]pyridine-1,3-dione were carried out according International Conference on Harmonization guidelines. For observation degradation tested compounds, RP-HPLC method was used. study included effect temperature, relative humidity, water, H+ OH– ions, hydrogen peroxide, light (6.0 × 106, 1.2 106 lux·h) stability derivatives. Studies have shown that these...

The series of three 4-alkoxy-2-[2-hydroxy-3-(4-aryl-1-piperazinyl)propyl]-6-methyl-1H-pyrrolo[3,4-c]pyridine-1,3(2H)-diones were synthesized. structures all formed compounds identified by elemental analysis, FTIR, and 1H NMR. synthesized studied using differential scanning calorimetry thermogravimetric analysis in order to determine the existence multiple solid-state forms. Our measurements showed that solvent, mechanical treatment, quenching are important factors. Two stable one metastable...

The new derivatives of 3,4-pyridinedicarboximide were synthesised. Experimental measurements carried out using 1H NMR spectra, IR elemental analyses and differential scanning calorimetry. purpose this study was to the thermal stability these four compounds establish a solid-state polymorphism. Measurements for samples obtained from ethanol n-hexane after long-time storage.

The present study aimed to design and synthesize a series of 2-hydroxy-3-(4-aryl-1-piperazinyl)propyl phthalimide derivatives, which are analogs 1H-pyrrolo[3,4-c]pyridine-1,3(2H)-dione derivatives with proven analgesic effect. In accordance the basic principle proposed by Lipinski's rule, probable bioavailabilities F1-F4 phthalimides were assessed. obtained values indicate good absorption after oral administration ability cross blood-brain barrier. four compounds differing in type...

The subject of the work was synthesis new derivatives of1H-pyrrolo[3,4-c]pyridine-1,3(2H)-dione with potential analgesic and sedative activity. Eight compounds werereceived. activity confirmed in “hot plate” test “writhing” test. All tested imides 8–15 were more active than aspirin, two them, 9 11, similar to morphine. In addition, all inhibited locomotor mice a statistically significant extent, them also prolonged duration thiopental sleep.On basis results obtained for previously...

The treatment of cancer represents one the most significant challenges currently facing modern medicine. search for new drugs that are effective in patients is an ongoing endeavor. It frequently case molecular target anticancer a DNA molecule. therapeutic effect drug achieved by influencing structure macromolecule or inhibiting its function. Among synthetic substances with potential effects, particular attention should be paid to phthalic acid imide derivatives. Three phthalimide derivatives...

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Five derivatives of 4‐alkoxy‐6‐methyl‐pyrrolo[3,4‐c]pyridine‐1,3‐dione were separated by TLC and HPLC methods using silica gel 60 F254 plates, analytical columns: LiChrosorb® RP‐8 (250×4 mm, 5 µm) LiChrospher® 100 RP‐18 µm), respectively. From the seven remaining mobile phases, three offered for use with two‐dimensional TLC. The values separation parameter (α), constant pair (RF α), ΔRF two neighbouring spots on each chromatogram defined. phase C (butan‐1‐ol–propan‐2‐ol–cyclohexane‐acetic...

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