Objective: Benzoxazole derivatives have antifungal, anticancer, antibacterial, and anticonvulsant function. Encouraged by this comment, we agreed to synthesize new Benzoxazole compounds connected to the bases of Schiff's. Methods: 2,4-diaminophenol (1) was prepared by the reaction of 2,4-dinitrophenol and sodium dithionate. Compound (1) reacted with either acetic acid to afford compound (2) or with formic acid to afford compound (3). The Schiff bases were preparation from the reaction condensing reaction of compound (2) or (3) and aromatic aldehydes or ketone; [p-nitrobenzaldehyde, p-hydroxybenzaldehyde, p-chlorobenzaldehyde, p-bromoacetophenone and terephthaldehyde]. Results: FTIR and 1H-NMR spectroscopy characterized all of the preparation compounds. The synthesized derivatives against (Gram positive bacteria GPB) (Bacillus subtilis) and two (Gram-negative bacteria GNB) (Klebsiella pneumoniae and Escherichia coli) and (one fungal species Candida albicans), have been evaluated to their antibacterial activity in vitro. all results showed which most of them have good antibacterial activity, while their antifungal activity revealed that compounds displayed slight antifungal activity. The synthesized Benzoxazole derivatives were docked using, glucosamine 6-phosphate synthase as a ligand. Conclusion: The antimicrobial activity indicates that compounds (4), (7) and (8) have more potent antibacterial activity than the compounds (5) and (6). Molecular docking study revealed that compounds (7) and (8), with bulky phenyl groups are essential to block the active centers of (GluN-6-Ps) amino acids synthase in the bacteria.
Heterocyclic 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 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
The work involves synthesis of new quinolin-2-one Schiff bases (XIII)a,b and (XIV)a,b, pyrazoles (XI)a,b and pyrazolines (XII)a,b derivatives containing isoxazoline or pyrimidine cycle starting with chalcones. 3-Aminoacetophenone was reacted with 4-bromobenzaldehyde or 4-N,N-dimethyl aminobenzaldehyde in basic medium to give chalcones (I)a,b by Claisen-Schemidt reaction. These chalcons were reacted with hydroxylamine hydrochloride or with thiourea in basic medium to form isoxazolines (II)a,b or pyrimidine-2-thion (III)a,b ,respectively.Also the pyrimidine-2-thiones (III)a,b and isoxazolines (II)a,b reacted with 4-or 3-substituted benzaldehyde and coumarin to form Schiff bases (IV)a-f (V)a-f and quinoline derivatives (VII)a-d(VIII)a-d, re
... Show MoreMefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-t
... Show MoreThis work includes synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1).10-nitrosyl phenoxazine was prepared through the reaction of phenoxazine with sodium nitrite to give compound (2), which reacted with zinc in acetic acid to give 10-amino phenoxazine (3). Condensation of compound (3) with benzoyl chloride, isovaleryl chloride and 4-bromophenacyl chloride gave 10-amido phenoxazine derivatives (4-6).
Series of new derivatives of quinoline-2-one were synthesized ,m-cresol was chosen as the starting material which was reacted with ethyl acetoacetate in presence of conc.sulphuric acid to give 4,7-dimethyl coumarin (I) which treated with nitric acid in the presence of sulpharic acid afforded 4,7-dimethyl-6-nitrocumarin (II) and 4,7-dimethyl-8-nitrocumarin (III) and then the compound (II) was treated with hydrazine hydrate80% to give a new compound 1-amino-4,7-dimethyl-6-nitroquinoline-2(1H)-one (IV).The latter compound was used to synthesize different
compounds via the reaction with aldehydic azo compounds (V-VII) by Schiff base reaction to prouduce compounds(VIII-X), these azo compounds were prepared by reaction of different aromatic
This work comprises the synthesis of new phenoxazine derivatives containing N-substituted phenoxazine starting from phenoxazine (1). Synthesis of ethyl acetate phenoxazine (2) through the reaction of phenoxazine with ethylchloroacetate, which reacted with hydrazine hydrate to give 10-aceto hydrazide phenoxazine (3), then reacted with formic acid to give 10-[N-formyl acetohydrazide] phenoxazine (4). Reaction of compound (4) with phosphorous pentaoxide or phosphorus pentasulphide to gave 10-[N-methylene-1,3,4-oxadiazole] phenoxazine (5) and 10-[N-methylene-1,3,4-thiadiazole] phenoxazine (6).
The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] an
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