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Synthesis, Antibacterial, and Molecular Docking Study of Novel 2-Chloro-8-Methoxy-3-Aryl-[1,3] Benzoxazine Derivatives using Vilsmeier Reagent
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Reducing of ethyl 4-((2-hydroxy-3-methoxybenzylidene)amino)benzoate (1) afford ethyl 4-((2-hydroxy-3-methoxybenzyl)amino)benzoate (2). Reaction of this compound with Vilsmeier reagent affords novel 2-chloro-[1,3] benzoxazine ring (3). The corresponding acid hydrazide of compound 3 was synthesized from reaction of compound (3) with hydrazine hydrate. Newly series of hydrazones (5a–i) were synthesized from reaction of acid hydrazide with various aryl aldehydes. Antibacterial activity of the hydrazones was secerned utilizing gram-negative and gram-positive bacteria. Compound (5b) and (5c) exhibited significant antibacterial ability against both gram-negative and gram-positive bacteria, while the compounds (5a) showed mild antibacterial activity. Compounds (5d–i) did not display notable activity. The molecular docking of synthesised compounds were tested inside the pocket of bacterial gyrase enzyme target site by using MOE 2015 software, which acts as Adenosine triphosphate (ATP)-binding domain bacterial gyrase enzyme pocket and novobiocin was used as reference.

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Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Barbiturate Derivatives of D-Erythroascorbic Acid
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 The   aim  of   this   work   is   the   synthesis  of   new   derivatives  of   barbiturate   of  D-erythroascorbic acid. To obtain these derivatives, the 5,6-O-isopropylidene-L-ascorbic acid (4) was chosen, which was prepared from the reaction of L-ascorbic acid (3) as a starting material with dry acetone in the presence of hydrogen chloride. The esterification of hydroxyl groups at C-2 and C-3 positions with excess of benzoyl chloride in dry pyridine was obtained compound (5). Hydrolysis for compound (5) in acetic acid (65%) gave the compound (6). Oxidation of the product (6) with sodium periodate results an Al

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Publication Date
Sun Mar 04 2018
Journal Name
Baghdad Science Journal
Synthesis and Characterization of a Molecularly Imprinted Polymer for Diclofenac Sodium Using (2-vinylpyridine and 2-hydroxyethyl metha acrylate) as the Complexing Monomer
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Four electrodes were synthesized based on molecularly imprinted polymers (MIPs). Two MIPs were prepared by using the diclofenac sodium (DFS) as the template, 2-hydroxy ethyl metha acrylate(2-HEMA) and 2-vinyl pyridine(2-VP) as monomers as well as divinyl benzene and benzoyl peroxide as cross linker and initiator respectively. The same composition used for prepared non-imprinted polymers (NIPs) but without the template (diclofenac sodium). To prepared the membranes electrodes used different plasticizers in PVC matrix such as: tris(2-ethyl hexyl) phosphate (TEHP), tri butyl phosphate (TBP), bis(2-ethyl hexyl) adipate (BEHA) and tritolyl phosphate (TTP). The characteristics studied the slop, detection limit, life time and linearity range of DF

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Publication Date
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Design, Synthesis and Preliminary Antimicrobial Evaluation of New Derivatives of Cephalexin
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There is a continuous and massive need for newer cephalosporins that should have resistance against β-lactamases and can be used orally. An approach of using cephalexin, as a well-studied and potent antibacterial compound is considered to prepare new designed derivatives.  These derivatives include the incorporation of amino acid moiety linked through an amide bond with the α-amino group of cephalexin. Certain aliphatic amino acids were used, such as glycine, alanine, valine and proline. The chemical structures of these derivatives were confirmed by IR spectroscopy and elemental analyses. All the synthesized compounds were subjected for preliminary evaluation of antimicrobial activity using well diffusion method, against certa

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Publication Date
Sat Sep 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Charact'erizatio.n of new Schiff base ligand [(2-{1-[(2 hydraxy­ benzylidene)-hydrazono]-ethyl} benzene-I, 3, 5--triol.] and it's CQmp.lexes. with Co en\ Ni . (U),, c·u(U)' and · zn(II).
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The eaction  of 2 4 .6-trihydroxyactophenonemonohydra1e  with

l hydr.azine monohydrate was realized ti·nder reflu.(( in methanol and i:l.

Jew drops of glacial acetic acid we.re added to give lhe'(int rmediate)

2-(1hydr pno-ctbyt)-benzcne-·1.3.5-r:Qql,       which      reacted     wittl

saEcy.laldehyde. jn methm)ql to gjy;e 'a new :tyRe CNzOi) Ligand  (H:flL]

f(2-{1-[(2-=bydroxy-bertzylide·ne)-bydrazqoo,J-e·thy.1}bcnze·neJ ;3·,5

of

 

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Publication Date
Wed Jan 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, characterization and bioactivity study of mixed-lig and complexes with some metal ions for new dithiocarbamate,3-aminophenol
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Publication Date
Sun May 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Novel Compounds Containing of Imidazolidinone and Oxazepine Rings
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The compound 3-[4Ì„-(4Ë­-methoxy benzoyloxy) benzylideneamino]-2-thioxo-imidazolidine-4-one [III] was prepared from the cyclization of thiosemicarbazone [II] with
ethyl α -chloroacetate in the presence of fused sodium acetate. Treatment the later compound
with acetic anhydride yielded the corresponding 1-Acetyl-3-[ 4Ì„- (4Ë­- methoxy benzoyloxy)
benzylideneamino] – 2 – thioxo -imidazolidine-4-one [IV]. 1,3-Oxazepine derivatives [V]a-d
and [VI]a-d are obtained from the reaction of compounds[III] and [IV] with different acid
anhydrides, in dry benzene. The FTIR and
1
HNMR spectroscopy are indicated a good
evidence for the formation of the synthesized compounds. Some of the synthesized

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Publication Date
Wed May 03 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Repeated Corrected Simpson's 3/8 Quadrature Method for Solving Fredholm Linear Integral Equations of the Second Kind
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  In this paper, we use the repeated corrected Simpson's 3/8 quadrature method for obtaining the numerical solutions of Fredholm linear integral equations of the second kind. This method is more accurately than the repeated corrected Trapezoidal method and the repeated Simpson's 3/8 method. To illustrate the accuracy of this method, we give a numerical example

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Publication Date
Mon Dec 29 1997
Journal Name
كلية العلوم للبنات
Synthesis And Studies Of Complexes Of Some Elements With 2-Mercaptohiazole (2-HMBT)
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Synthesis And Studies Of Complexes Of Some Elements With 2-Mercaptohiazole (2-HMBT)

Publication Date
Mon Jul 01 2019
Journal Name
Journal Of Physics: Conference Series
Effect of Nickel Substitution On Structural and Electrical Properties of Hg<sub>0.5</sub>Pb<sub>0.5</sub>Ba<sub>2</sub>Ca<sub>2</sub>Cu<sub>3-y</sub>Ni<sub>y</sub>O<sub>8+δ</sub> Superconductor Composite
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Abstract<p>six specimens of the Hg<sub>0.5</sub>Pb<sub>0.5</sub>Ba<sub>2</sub>Ca<sub>2</sub>Cu<sub>3-y</sub> <italic>Ni<sub>y</sub> </italic>O<sub>8+δ</sub> (y=0.2,0.4,0.6,0.8,1.0) superconducting compound were prepared by solid state reaction method, with sintering temperature equal to 1123K for 24 hours. The electrical resistivity was examined by the four probe technique, It was found that all the specimens have metallic behavior and increasing the critical temperature with increasing nickel concentration. The optimum critical temperature T<sub>c</sub> was found equal </p> ... Show More
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Publication Date
Fri Jul 05 2013
Journal Name
Pharmacie Globale International Journal Of Comprehensive Pharmacy
SYNTHESIS OF NEW PROPRANOLOL DERIVATIVES AS POSSIBLE PRODRUGS
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Propranolol is a nonselective-adrenergic blocker used in the treatment of hypertension, cardiac arrhythmias, and angina pectoris. A significant problem in propranolol therapy is that it undergoes extensive presystemic metabolism after oral administration leading to reduced bioavailability. In this study, two new propranolol derivatives have been designed, synthesized and characterized. These compounds were formed by acylation of propranolol followed by nucleophilic substitution reaction of acylated propranolol, these derivatives were analyzed for IR, CHN, melting points, and evaluated for their lipophilic properties compared with propranolol. The lower partition coefficient of these two derivatives revealed that the prodrug approach may be

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