Synthesis, biomedical activities, and molecular docking study of novel chromone derivatives
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Investigation of mesomorphic properties of new 1,3,4-thiadiazolines (which are synthesised via many steps in Scheme 1) was carried out in this study. These compounds are designed to have a heterocyclic unit, a carboxylate linkage group and a polar ether chain at the end of the molecule adjacent to the benzene ring, which enhance the dipolar interactions forces (varied from one to eight carbons) to investigate the association properties of their phases. The structure of the target compounds and the intermediates were confirmed by 1H NMR, 13C NMR, mass and FTIR spectral techniques. Polarised microscopic studies revealed that all the compounds in the series exhibited enantiotropic liquid crystalline properties. This was further confirmed using
... Show MoreThis research included the preparation of 2-mercaptobenzoxazole (N1) by the reaction of ortho-aminophenol with carbon disulfide in an alcoholic potassium hydroxide solution. The 2-mercapto benzoxazole (N1) was then treated with hydrazine to obtain the 2-hydrazino benzoxazole (N2). A number of hydrazones (N3-N5) were prepared through the reaction of N2 with different benzaldehydes. The compound (N6) was also prepared whereby the ring closing of hydrazone (N3) using chloroacetylchloride, while the compound (N7) was prepared by treating 2-hydrazino benzoxazole with acetylacetone. When the compound (N1) was treated with formaldehyde, it afforded the compound (N8). Also, the N9 was obtained from the reaction of N1 with chloroacetic acid in th
... Show MoreNew substituted coumarins derivatives were synthesized by using nitration reaction to produce different nitro coumarin isomers which were separated from these isomers by using different solvent, and the reduction of nitro compounds was done to give corresponding amino coumarins. Temperature and reaction time of reaction were very important factors in determining the most productive nitro isotopes. A low temperature for three hours was sufficient to give a high product of a compound 6-nitro coumarin while increasing the temperature for a period of twenty-four hours that gave a high product of 8-nitro-coumarin. The synthesized compounds were confirmed by FT-IR,1 H-NMR, and13 C-NMR spectroscopy and all final compounds were tested for their ant
... Show MoreObjective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the anticancer activities. Methods: Baclofen was initially reacted with aromatic aldehydes to create Schiff base derivatives (Ia–Ib), which were then closed in the next step using anhydrous acids to form oxazepine derivatives (IIa–IId). Results: The title compounds were synthesized successfully and identified using FT-IR, 1H NMR, and 13C NMR spectroscopy. Additionally, compound (IIc)’s (3-(4-chloro-phenyl)-4-[2-(4nitro-phenyl)-4,7-dioxo-4,7-dihydro-[1,3] oxazepin-3-yl]butyric acid) anticancer activity was assessed using MTT assay against FTC-133 (thyroid cancer) compared with WRL-68 (normal cell line). Discus
... Show MoreHeterocyclic polymers / silica nanocomposite one of important materials because of excellent properties such as thermal , electrical , and mechanical properties , so that hybrid nanomaterial are widely used in many fields, in this paper nanocomposite had prepared by modification of silica nanoparticals by using acrylic acid and functionalized the surface of nanoparticles, and using free Radical polymerization by AIBN as initiators and anhydrous toluene as solvent to polymerize functionalize silica nanoparticles with heterocyclic monomers to prepare heterocylic polymers / silica nanocomposite and study electrical conductivity , The nanocomposite which had prepared characterized by many analysis technique to study thermal properties such
... Show MoreNitrogen heterocycles are of a special interest because they constitute an important class of natural and non natural products, many of which exhibit useful biological activities.Among these nitrogen heterocycles are 1, 3, 4-thiadiazole containing compounds. The therapeutic effects of these derivatives have been well studied for a number of pathological conditions including inflammation, pain, or hypertension. Moreover, synthesis of thiadiazoles has attracted wide-spread attention due to their diverse applications as antibacterial, anticancer, antifungal anti-inflammatory and antidepressant agents.According to this information’s new derivatives of 1, 3, 4-thiadiazole were designed and synthesized and in the hope of having some act
... Show MoreIn this research, cyclic compounds derived from 2- furfural mercaptan (oxazole, triazoles) were synthesized, and their biological efficacy was measured and compared with standard drugs. Also, their effectiveness as anti-oxidant was measured and compared with ascorbic acid as a standard substance. Some of the synthesized compounds were deduced with good efficacy. © 2021 Sami Publishing Company. All rights reserved
In this work, the preparation of some new oxazolidine and thiazolidine derivatives has been conducted. This was done over two steps; the first step included the synthesis of Schiff bases A1-A5 in 72-88% yields by the condensation of isonicotinic acid hydrazide and aldehydes. The second step includes the cyclization of derivatives A1-A5 with glycolic acid and thioglycolic acid to obtain the desired products, oxazolidine derivatives B1-B5 (44-60% yields) and thiazolidine derivatives C1-C5 (41-61% yields), respectively. The structure of the prepared compounds was characterized using FT-IR, 1H NMR, and 13C NMR spectroscopy. Some of the produced compounds were tested for antioxidant properties.
The present work involved synthesis of new thiozolidinone derivatives,These derivatives could be divided into three type of compounds; quinolin-2-one[V]a,b ,Schiff bases[VI]a,b and imide compounds[VII]a-d. The reaction p-Hydroxyacetophenone with thiosemicarbazide led to formation thiosemicarbazon compound [II], the reacted of thiosemicarbazone with chloro acetic acid in CH3CO2Na led to yield 4- thiazelidinone compound[III] in addition, thiosemicarbazide was POCl3 to [III] give [IV] compound used intermediates to synthesis new compounds of reacted with two type of coumarin in glacial acetic acid to give quinolin-2-one[V]a,b, The later compound refluxing with different benzaldehyde in dry benzene and glacial acetic acid give Schiff bases[VI]a
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