In this work, a series of new Nucleoside analogues (D-galactopyranose linked to oxepanebenzimidazole moiety) was synthesized via multisteps synthesis. The first step involved preparation of two benzimidazoles 2-styrylbenzimidazole and 2-(phenyl ethynyl) benzimidazole via reaction of phenylenediamine with cinnamic acid or ?-phenyl propiolic acid. Electrophilic addition of the prepared benzimidazoles by three anhydrides in the second step afforded (4-6) and (14-16) which in turn were treated with 1,2,3,4-di-O-isopropylidene galactopyranose in the third step to afford a series of the desirable protected nucleoside analogues (7-9) ,(17-19)which after hydrolysis in methanolic sodium methoxidein the fourth step afforded the free nucleoside analogues (10-12) and (20-22) .The synthesized compounds were identified by FT-IR and some of them by 1H-NMR and13C-NMR. The synthesized oxepane nucleoside analogues were screened for their antibacterial activity against three types of bacteria including Staphylococcusaureus ,Bacillus(gram positive) andE.coli (gram negative) bacteria repectively.
Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very
... Show MoreThe antimicrobial potency of the crude ethanolic extracts from different Iraqi plants were evaluated . Further more, total sesquiterpene lactones and phenolic compounds were isolated and their antimicrobial activity attempted. The results indicated that crude extracts have no activity except that of Callistemon lanceolatus. Also, the sesquiterpene lactones and phenolic compounds isolated from Callistemon lanceolatus were the most significant antimicrobial active constituents of the studied plants.
ليكاند ازو جديد. 4-((3-formyl-2-hydroxyphenyl)diazenyl)-N-(5-methylisoxazol-3-yl)benzenesulfonamide, الليكاند المحضر استعمل لتحضير معقدات من ايونات معادن مختلفة مثل الكروم الثلاثي والمنغنيز الثنائي والحديد الثلاثي والبلاديوم الثنائي بنسب مولية (1:1) ( ليكاند : فلز) نتائج التشخيص للمركبات يتقنيات مطيافية الاشعة فوق البنفسجية الاشعة تحت الحمراء الرنين النووي المغناطيسي البروتوني والكربوني وطيف الكتلة والتحليل الدقيق للعناصر ومحتوى الفلز وال
... Show MoreA novel ligand, (E)-5-((2-hydroxy-4,6-dimethylphenyl)diazenyl)-2,3-dihydrophthalazine-1,4- dione, was synthesized through the reaction of 3,5-dimethylphenol with the diazonium salt of 5-amino-2,3-dihydrophthalazine-1,4-dione. The ligand underwent characterization through the utilization of diverse spectroscopic methods, including UV-Vis, FT-IR, 13C, and 1H-NMR, alongside Mass spectroscopy and micro elemental analysis (Carbon, Hydrogen, Nitrogen, and Oxygen). Metal chelates of transition metals were prepared and analyzed using elemental analysis, mass spectra, atomic absorption, UV-Vis, FT-IR spectral analysis, as well as conductivity and magnetic measurements. The investigation into the compounds’ nature was conducted by utilizing mole r
... Show MoreFour batches of sertraline HCl microspheres were prepared using a poly (D-L-lactide-co-glycolide) (PLGA) polymer ( Mw. 9, 27, 30 and 83 KDa) as a delivery system. The microspheres were prepared by a dispersion/solvent extraction-evaporation method and characterized for drug loading by UV, particle size by laser diffractometry and surface morphology by scanning electron microscopy (SEM). The in vitro sertraline HCl release was studied. Spherical microspheres with a mean diameter of 21 to 26 µm loaded with 24.6 – 38.2% were produced. The in vitro drug release was shown to be depend on polymer molecular weight and also on the drug loading. Differential scanning calorimetry (DSC) was employed to investigate the physical state
... Show MoreMetal complexes of Mn(II), Co(II), Ni(II), Cu(II), Cd(II), Zn(II), Hg(II), Pd(II), and Pt(II) with Schiff base ligand (LH) derived from 2,5-dichloroaniline and 2-hydroxy-5-metheylbenzalaldehyde were synthesized and characterized using a variety of spectrophotometric techniques The findings of the spectroscopic analysis indicated that (LH) behaved as a binary coordinating agent to the metal ion by the N and O atoms, and the geometry shape of the complexes was octahedral, with the exception of the Pd and Pt complexes, which had a square planar geometry. Using the DPPH radical scavenging method, we investigated the antimicrobial activity of the compound against Staphylococcus aureus and Escherichia coli, as well as the antifungal activity of t
... 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 MoreReaction of,2- [( 4- amio phenyl ) diazenyl] 1,3,4- thiadiazole -5- thiol (S1) with p- chlorobenzeldehyde,3,4 – dimethoxy benzaldehyde and pyrrol-2- carbonxaldehyde gave -5- [{4-(4-chlorobenzylidene amino) phenyl} diezenyl]-1,3,4- thiadiazole-2- thiol (S2),5-[{ 4-[(3,4- dimethoxybenzyldene )amino phenyl ] diazenyl)-1,3,4- thiadiazole-2-thiol,(S3) and -5- [4-(1,H – pyrrol -2- yl- methylene)amino phenyl] diazenyl)-1,3,4- thiadiazole-2- thiol (S4) respectively as schiff's bases compounds. On the same route-2-[(4-amino-1- naphthyl ) diazenyl] -1,3,4- thiadiazole -5- thiol (S5) reacts with –p- chloro benzaldehyde and –m- nitrobenzaldehyde to give the follwing schiff's bases -5-[{ 4-(4- chloro benzylidene ) amino -1- naphthyl} diazenyl]
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