Synthesis, biomedical activities, and molecular docking study of novel chromone derivatives
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By unusual method for separating two isomers of a substituted nitro-coumarin using a soxhlet extractor and in controlling temperature to get a selective nitration reaction, several new Schiff base coumarins were synthesized from nitro coumarins as starting material, which were reduced by Fe in glacial acetic acid to produce corresponding amino coumarin derivatives. Then the latter was reacted with different aromatic aldehydes to produce the desired Schiff bases derivatives. After characterization by Fourier transform infrared (FT-IR), Proton nuclear magnetic resonance (1HNMR) and Carbon-13 nuclear magnetic resonance (C-NMR), all these compounds were evaluated as potential Antimicrobial and Antioxidant Agents.
Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w
... Show MoreA new Schiff base ligand [2,3,8,9–tetra -phenyl-1,4,5,7,10,12-hexa azo-5,12- dihydro -6,11- dione 1,3,7,10-dudec-tetra-ene] [H2L] and its complexes In general formula [M(H2L)]Cl2 (where : M= CoII, NiII, and PdII) were prepared. This ligand was prepared in two steps,in the first step a solution of benzil in methanol was reacted under reflux with semicarbazidhydrochlorid to give an (intermediate compound)[benzyl bis–(Semicarbazone)] which was reacted in the second step with benzil giving the mentioned ligand. The
... Show MoreEye loss may be caused as a result of eye trauma, accidents, or malignant tumors, which leads the patient to undergo surgery to remove the damaged parts. This research examines the potential of computer vision represented by Structure from Motion (SfM) photogrammetry in fabricating the orbital prosthesis as a noninvasive and low-cost technique. A low-cost camera was used to collect the data towards extracting the dense 3D data of the patient facial features following Structure from Motion-Multi View Stereo (SfM-MVS) algorithms. To restore the defective orbital, a Reverse Engineering (RE) based approach has been applied using the similarity RE algorithms based on the opposite healthy eye to rehabilitate the defected orbital precisely
... Show More4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic
... Show MoreA new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Fina
... Show MoreA new class of thiadiazole /silica nanocomposites with chemical bonds between thiadiazole monomers and modified nanosilica surface were synthesized by free radical polymerization. Presence silica nanoparticles in the structure of nanocomposite showed effectively improve the physical and chemical properties of Producing polymers. A nanocomposite material with feature properties comparison with their polymers, The structure and morphology of the synthesis materials were investigated by FT-IR spectrum which display preparation new thiadiazole compounds and polymerization monomers. FT-IR showed disappeared double bond (C=C) of monomers, due to produce long chains of thiadiazole polymers and nanocomposite. X-ray diffraction gave idea ab
... Show MoreThis new azo dye 3-((2-(1H-indol-3-yl) ethyl) diazenyl) quinoline-2-ol was subsequently used to prepare a series of complexes with the metal ions of Cr+3, Cu+2, VO+2, Mn+2and Mo+6. The compounds identified by 1H and 13C-NMR, FT-IR, UV-Vis, mass spectroscopy, as well as TGA, DSC, and C.H.N., conductivity, magnetic susceptibility, metal and chlorine content. The results showed that the ligand behaves in a bidantate, and that the complexes gave octahedral, excepting for VO+2 square pyramid was given, that all complexes are non-electrolytes. The effectiveness of mention the compounds in inhibiting free radicals was evaluated by the ability to act as an antioxidant was measured using DPPH as a free radical and gallic acid as a standard s
... Show MoreCurrent research included preparation, characterization of some new chitosan- hydroxy benzaldehyde-Schiff bases with maleic anhydride. The present study aimed to the synthesis and characterization of novel chitosan Schiff base compounds using para- hydroxy benzaldeh and maleic anhydride. The derivative of the schiff-chitosan base, which is associated with different drugs, has been replaced with different amino and hydroxy drugs. The derivative is characterized by different analytical techniques. The results of FT-IR studies clearly indicate construction of the chief amine group in chitosan and the emergence of new bands that correspond to the association of maleic anhydride with the chitosan base. TGA, 1
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