86503-94-8Relevant academic research and scientific papers
Docking Study, Synthesis, and Anti-Inflammatory Potential of Some New Pyridopyrimidine-Derived Compounds
Abdelgawad, Mohamed A.,Al-Sanea, Mohammad M.,Azouz, Amany A.,Bakr, Rania B.,El-Damasy, Ashraf K.,Elmowafy, Mohammed,Ghoneim, Mohammed M.,Musa, Arafa
, p. 451 - 463 (2022/02/05)
Background and Purpose: Because of gastrointestinal irritation and kidney toxicity associated with non-steroidal anti-inflammatory drugs and the cardiovascular problems of Coxibs use, developing novel anti-inflammatory agents with reduced toxicity and improved selectivity remains a major challenge. Depending on our previous work, a novel series of pyridopyrimidinones IIIa-i has been synthesized via reaction of 6-amino-2-thioxo-2,3-dihydro-1H-pyrimidin-4-one (I) and phenyldiazenyl aromatic aldehydes (IIa-i). All the new constructed compounds were fully characterized by elemental and spectral analysis. Methods: The target compounds IIIa–i were investigated for their potential towards COX inhibition, anti-inflammatory properties using carrageenan induced edema model in rat paw, and the ulcer indices of the most active members. Results: The ethyl pyridopyrmidinone-benzoates IIIf, IIIg and IIIh showed superior inhibitory activity of carrageenan induced edema to celecoxib. Furthermore, the pyridopyrimidinones IIId, IIIf, IIIg, and IIIi exerted improved COX-2 inhibitory activity (IC50 = 0.67–1.02 μM) comparing to celecoxib (IC50 = 1.11 μM). Moreover, the gastric ulcerogenic potential assay of compounds IIIf– h revealed their lower ulcerogenic liability than indomethacin with comparable effect to celecoxib. Conclusion: Virtual docking investigation of the most active candidates IIId, IIIf, IIIg and IIIi in the active site of COX-2 enzyme showed that these compounds implied interaction and binding motif similar to the cocrystallized ligand bromocelecoxib.
Effect of Structure of Photoresponsive Molecules on Photochemical Phase Transition of Liquid Crystals I. Synthesis and Thermotropic Properties of Photochromic Azobenzene Derivatives
Ikeda, T.,Miyamoto, T.,Kurihara, S.,Tsukada, M.,Tazuke, S.
, p. 357 - 371 (2007/10/02)
Seventeen azobenzene derivatives were synthesized and their thermotropic properties were examined.They are classified into three groups.In the first group, 4-cyanobiphenyl moieties are attached to both sides of azobenzene through various alkyl spacers: AB(nCB)2 where n = 3, 4, 5 and 6.In the second group, the 4-cyanobiphenyl moiety is attached to one side of the azobenzene, while the substituent of the other side was kept as OCH3:1ABnCB, where n = 3, 4, 5, 6 and 8.The third group is the azobenzene derivatives which possess alkoxy substituents at both para positions of azobenzene (nABm) or at various positions of the azobenzene phenyl rings (k,1ABn,m).The introduction of the 4-cyanobiphenyl group at the end(s) of the molecules is based on the attempt of highly efficient photochromic molecules to induce photochemical phase transition of liquid crystals by providing the photochromic trigger molecules with high affinity to the host liquid crystal.Both 1ABnCB and AB(nCB)2 exhibited the liquid crystalline phases, whereas among nABm and k,1ABn,m, only 1AB8 and 8AB8 showed the liquid crystalline phase.The 1ABnCB series exhibited a distinct odd-even variation in phase transition temperatures as well as enthalpy and entropy changes with the length of the flexible spacers, while the AB(nCB)2 series did not show clear odd-even variation except for the liquid crystal to isotropic phase transition temperatures.
