Levofloxacin belongs to the fluoroquinolone family; it is a potent broad-spectrum bactericidal agent. The pharmacophore required for significant antibacterial activity is the C-3 carboxylic acid group and the 4-pyridine ring with the C-4 carbonyl group, into which binding to the DNA bases occur. In this work, we tried to show that by masking the carboxyl group through amide formation using certain amines to form levofloxacin carboxamides, an interesting activity is kept. Levofloxacin carboxamides on the C-3 group were prepared, followed by the formation of their copper complexes. The target compounds were characterized by FT-IR, elemental analysis. The antimicrobial activity of the target compounds was evaluated and showed satisfactory results compared with levofloxacin. This has indicated that the presence of the carbonyl of C-3 carboxyl moiety is not essential, as levofloxacin carboxamides showed interesting copper complexes indicating that they retain the activity of levofloxacin, since its activity depends on binding to DNA gyrase via magnesium binding
Unregulated epigenetic modifications, including histone acetylation/deacetylation mediated by histone acetyltransferases (HATs) and histone deacetylases (HDACs), contribute to cancer progression. HDACs, often overexpressed in cancer, downregulate tumor suppressor genes, making them crucial targets for treatment. This work aimed to develop non‐hydroxamate benzoic acid–based HDAC inhibitors (HDACi) with comparable effect to the currently four FDA‐approved HDACi, which are known for their poor solubility, poor distribution, and significant side effects. All compounds were structurally verified using FTIR, 1HNMR, 13CNMR, and mass spectrometry. In silico ana
The new Hexadentate complexes type [M(H3L3)]K were prepared from the condensation reaction of Diphenylmonoxime and KOH with (Mn(II), Co(II), Ni(II), Cu(II), Zn(II), and Hg(II)) in methanol with 3:1 ligand : metal ratio to give a series of new complexes of the general formula [M(H3L3)]K (where: M(II) = Mn ,Co ,N ,Cu ,Zn and Hg).All compounds have been Characterized by spectroscopic methods [I.R, U.v-Vis, atomic absorption and microanalysis (C.H.N) along with conductivity measurements. The stability constant K and Gibbs free energy ∆G were calculated for [Co (H3L3)] K, [Ni (H3L3)] K and [Cu (H3L3)] K and complexes using spectrophotometer method. The obtained values indicate that these complexes stable in their solution. From the above data
... Show MoreThe Chemistry of heterocyclic sulphur and nitrogen containing compounds have a great role in the field of scientific studies, The 2-amino 5-mercapto-1,3,4-thiadiazole ring for instance, has gained more importance in recent years because they are considered as potent biologically active nucleus. In this study disulfide derivative can be obtained by oxidation with hydrogen peroxide of thiol group of the heterocyclic 2-amino 5-mercapto-1,3,4-thiadiazole ring to obtain compound (3) with expected antibacterial activity. In order to use it as a diazo component to prepare some new bis azo compounds as possible antibacterial agents, the reaction of two primary amino groups on both sides of disulfide dimer with sodium nitr
... Show MoreIn the present research synthesis and study of biological activity a series of new polymers modified of chitosan with compounds containing azo group. Beginning diazonium salt produced from 3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diamine reacted with concentrated HCl acid and sodium nitrite. The coupling reaction between diazonium salt with substituted aromatic aldehyde to produce Azo derivatives )1-6(. Azo Schiff bases Chitosan )7-12( were synthesized by condensation of Chitosan with Azo derivatives )1-6( in ethanol with some drops of glacial acetic acid. The structural modifications of Chitosan ring (linked to a bioactive azo moiety) were expected to give new derivatives )7-12( with a diverse range of biological functions. These compounds' st
... Show Moreفي البحث الحالي تم تحضير ودراسة النشاط الحيوي لسلسلة من البوليمرات الجديدة المحورة من الكيتوسان مع مركبات تحتوي على مجموعة الآزو. في البداية تم تحضير ملح الديازونيوم من تفاعل 3,3'-dimethyl-[1,1'-biphenyl]-4,4'-diamine مع حامض الهيدروكلوريك المركز ونتريت الصوديوم .ثم تفاعل الازدواج بين ملح الديازونيوم مع الديهايدات اروماتية معوضة لإنتاج مشتقات الازو (1-6). ازو شف بيس كيتوسان((12-7 والتي حضرت من تفاعل الكيتوسان مع مشتقات
... Show MoreTransition metal complexes of Y(III), La(III) and Rh(III) with azo dye 2,4-dimethyl-6- (4-nitro-phenylazo)-phenol derived from 4-nitroaniline and 2,4-dimethylphenol were synthesized. Characterization of these compounds has been done on the basis of elemental analysis, electronic data, FT-IR,UV-Vis and 1HNMR, as well as conductivity measurements. The nature of the complexes formed were studies following the mole ratio and continuous variation methods, Beer's law obeyed over a concentration range (1x10-4- 3x10-4). High molar absorbtivity of the complex solutions were observed. From the analytical data, the stoichiomerty of the complexes has been found to be 1:3 (Metal:ligand). On the basis of Physicochemical data octahedral geometries were as
... Show More. New Schiff base ligand 2-((4-amino-5-(3, 4, 5-trimethoxybenzyl) pyrimidin2-ylimino) (phenyl)methyl)benzoic acid] = [HL] was synthesized using microwave irradiation trimethoprim and 2-benzoyl benzoic acid. Mixed ligand complexes of Mn((ІІ), Co(ІІ), Ni(ІІ), Cu(ІІ), Zn(ІІ) and Cd(ІІ) are reacted in ethanol with Schiff base ligand [HL] and 8-hydroxyquinoline [HQ] then reacted with metal salts in ethanol as a solvent in (1:1:1) ratio. The ligand [HL] is characterized by FTIR, UV-Vis, melting point, elemental microanalysis (C.H.N), 1H-NMR, 13C-NMR, and mass spectra. The mixed ligand complexes are characterized by infrared spectra, electronic spectra, (C.H.N), melting point, atomic absorption, molar conductance and magnetic m
... Show MoreThree cultivars of the crop Almash (Green Indian VC6089A10, Green Indian VC6173B1319, and Black Indian Gold Star) were tested in a field experiment during the 2022 growing season in Ramadi, Anbar province, to determine the impact of spraying levels of zinc (0, 25, and 50) mg Zn L-1 and manganese (0, 30, and 60) mg Mn L-1 on some growth characteristics. The experiment was conducted using a randomized complete block design (RCBD) with three replicates, with each treatment being tested in a separate split plot. The study found that there were statistically significant differences between zinc levels, with the level giving 50 mg Zn L-1
This work includes preparation of Az, Qz, and Tz derivatives from the reaction of Schiff base (Sb) derivative with anthranilic acid, chloroacetyl chloride, and sodium azide, as well as, the characterization via FT-IR, 1H-NMR, and 13CNMR. The anticorrosion inhibition of these compounds was studied and the measurements of carbon steel (CS) corrosion in sodium chloride solution 3.5% (blank) and inhibitor in solutions were calculated at a temperature range of 293-323 K by the technique of electrochemical polarization. In addition, some thermodynamic and kinetic activation parameters for inhibitor and blank solutions (Ea⋇, ΔH⋇, ΔS⋇, and ΔG⋇) were determined. The results showed high inhibition efficacy for all the prepared compounds,
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