In vitro and in silico evaluation of 4'-hydroxy-[1,1'-biphenyl]-4-carbohydrazide Schiff base and oxadiazole derivatives targeting EGFR allosteric site
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Publication Date
Thu Jun 01 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Synthesis, Characterization, Biological and Antioxidant estimation of Mixed Schiff Base Ligand and Heterocyclic Compound with Some Metal ions
In this research, a group of complexes were prepared which were derived from Schiff base ligands, which is called (1E,1'E)-1,1'-(1,2-phenylene)bis(N-(2,4-dichlorophenyl) methanimine) (L) with ortho-phenanthroline (o-phen).The prepared complexes areM(II) [Co(II),Ni(II),Cu(II), Zn(II), Cd(II),and Hg(II)].A range of spectroscopic and technical techniques have been used to characterizethese materials, including:The FTIR, 1H-NMR, LC-Mass Spectrum, UV-Visbale, molar conductance, and magnaticmoment, atomic absorbtion, chlorid contents. Spectral results obtainedare showen that (ortho-phen) and (L) behave as neutral coordinating to the central metal ion by the donatingatoms(N2)of the both compounds. The geometry sha
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Publication Date
Sun Sep 15 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and In vitro/Ex vivo Evaluation of Nanoemulsion-Based in Situ Gel for Intranasal Delivery of Lasmiditan
Ex-vivo permeation study
Nanoemulsion
Intranasal
in situ gel
and Lasmiditan
Lasmiditan (LAS) was formulated as a nanoemulsion based in situ gel (NEIG)with the aim of improving its oral bioavailability via application intranasally. The solubility of LAS in oils, emulsifiers, and co-emulsifiers was determined to identify nanoemulsion (NE)components. Phase diagrams were constructed to identify the area of nanoemulsification. LAS NE was formulated using the spontaneous nanoemulsification method. Four NEs (F19, F24, F31, and F34) containing 7-15 % oleic acid (OA) as an oily phase, 40-55% labrasol (LR), and transcutol (TC) as emulsifier mixture at (1:1), (2:1), (3:1), and (1:2) ratio with 30-53 % (w/w) aqueous phase, having suitable optical transparency of 95–98%, globule size of 104-140 nm and polydisper
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Publication Date
Sat Sep 01 2018
Journal Name
Polyhedron
Novel dichloro (bis {2-[1-(4-methylphenyl)-1H-1, 2, 3-triazol-4-yl-κN3] pyridine-κN}) metal (II) coordination compounds of seven transition metals (Mn, Fe, Co, Ni, Cu, Zn and Cd)
The 1
3-dipolar cycloaddition “click” reaction between an azide and an alkyne to give a 1
2
3-triazole was reported by Huisgen in 1961 [1]. In 2002 the Copper(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) to prepare a 1
2
3-triazole was reported [2]
[3]. The existence of relatively basic nitrogen atoms in the 1
2
3-triazole rings
and the possibility of introducing additional donor groups in the substituents (Fig. 1)
made the CuAAC “click” reaction an attractive method to prepare differently substituted 1
2
3-triazoles. These compounds have been used as ligands to coordinate to various metal ions that display a range of applications such as in electrochemical and photochemical studies
in supramolecular chemistry
magnetism
metal-ion sensing and catalysis [4]. The reasons for the success of the “click” reaction
is that it is easy to carry out and is widely applicable. It is not affected by a variety of functional groups
and can be carried out with a variety of Cu(I) catalysts and solvents
including aqueous conditions. The Cu(I) catalysts overcome the high activation energy barrier of the non-catalyzed Huisgen reaction by changing the mechanism of the reaction. A large variety of copper catalysts can be used for the CuAAC reaction
on condition that the maximum concentration of Cu(I) species is generated during the reaction. The pre-catalyst can be a Cu(II) salt (usually CuSO4) together with a reducing agent (often sodium ascorbate) or a Cu(I) compound in the presence of a base or amine ligand and a reducing agent to prevent oxidation to Cu(II). Some strong oxidising cupric salts or complexes such as Cu(OAc)2 also work. The solvent is very flexible from organic to aqueous
with the most commonly used combination water + an alcohol (t-BuOH
MeOH or EtOH). The key role of the solvent or solvent mixture is to solubilize the substrates and Cu(I) catalyst in order to ensure rapid reactions. Such aqueous conditions are very useful for biochemical conjugations
as well as for organic syntheses.
We recently reported on the synthesis of a series of differently substituted 1
2
3-triazole chromophores
the substituted 2-(1-phenyl-1H-1
2
3-triazol-4-yl)pyridine ligands [5]
see Fig. 2 middle
with substituents R = H (L1)
CH3 (L2)
OCH3 (L3)
COOH
F
Cl
CN
CF3
O(CH2)3CH3 and N(CH3)2. These versatile ligands were found to coordinate to various first row transition metals
such as manganese
cobalt and nickel [6]. Here we extend the series to include more first row transition metal(II) coordination compounds
iron
copper and zinc
as well as a second row transition metal(II) coordination compound
cadmium
containing the 2-(1-(4-methyl-phenyl)-1H-1
2
3-triazol-1-yl)pyridine chromophore (Fig. 2 right with R = CH3). This series of seven novel coordination compounds is the first series of pyridyl-triazole based transition metal coordination compounds where seven different transition metals are coordinated to the same 1
2
3-triazole chromophore
namely 2-(1-(4-methyl-phenyl)-1H-1
2
3-triazol-1-yl)pyridine.
Publication Date
Sat Jul 22 2023
Journal Name
Journal Of Engineering
Removal of 4-Chlorophenoles from Simulated Wastewater by Advanced Oxidation Processes
4-chlorophenol
advance oxidation process
Fenton process
photo-Fenton process
UV photolysis.
The degradation and mineralization of 4-chlorophenol (4-CP) by advanced oxidation processes (AOPs) was investigated in this work, using both of UV/H2O2 and photo-Fenton UV/H2O2/Fe+3 systems.The reaction was influenced by the input concentration of H2O2, the amount of the iron catalyst, the type of iron salt, the pH and the concentration of 4-CP. A colored solution of benzoquinon can be observed through the first 5 minutes of irradiation time for UV/H2O2 system when low concentration (0.01mol/L) of H2O2 was used. The colored solution of benzoquinon could also be observed through the first 5 minutes for the UV/H2O2/Fe+3 system at high
concentration (100ppm) of 4-CP. The results have shown that adding Fe+3 to the UV/H2O2 system enhanced
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Publication Date
Sun Jun 05 2011
Journal Name
Baghdad Science Journal
Synthesized azodyes of 2-amino-1, 3, 4- thiadiazole - 5 - thiol
Several azo dyes were synthesized through coupling reaetion of some substituted phenols and B.naphthol with diazonium salt of 2- amino-1,3-4- thiadiazol -5- thiol. All the synthesized compounds during this work were characterized using some speetral data (F.TIRand UV)andM.P . 2-[4 --Hydroxy napthyl-azo ] -1,3,4-Thiadiazol -5-Thiol • 2- [2-- hydroxy –4- NO2 – phenyl- azo]- 1,3,4 - Thiadiazol –5-Thiol. • 2- [3--Amino-4-Hydroxy phenyl –azo]-1,3,4 - Thiadiazol –5-Thiol. . • 2-[2--Amino-4-Hydroxy phenyl -azo]-1,3,4 - Thiadiazol –5-Thiol . • 2- [3--Amino-6- Hydroxy phenyl -azo]-1,3,4 - Thiadiazol –5-Thiol. • 2-[2-- Hydroxy- 5 – chloro – Pheny - azo]- 1,3,4 - Thiadiazol –5-Thiol . • 2- [4-- Hydroxy phenyl -azo] -1,
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Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of Polyimides derived from 2,6-diamino-4-methyl-1,3,5-triazine
": 2
6- diamino -4-methyl-1
3
5-triazine
polyacryloyl chloride
polyimides derivatives ."
This work included synthesis of several new polymers of polyacryloyl chloride in two steps . The first step the included the reaction of N-( sub. or un sub. benzoyl and sub. or un sub. acetyl ) amidyl sub. 2,6- diamino -4-methyl-1,3,5-triazine (1-5) by condensation of many substituted acid chlorides with 2,6- diamino -4-methyl-1,3,5-triazine . While the second step included the reaction of polyacryloyl chloride with the produced compounds (1-5) in step (1) in the presence amount triethyl amine (Et3N) to obtain new polyimides (6-10). The prepared compounds were characterized by UV. , FT-IR, and some of them by 1H-NMR and 13C- NMR spectroscopy.
Publication Date
Thu Jun 25 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activity Evaluation of New Indole-Based Derivatives
N-acyl hydrazone
Indole-3-propionic acid
antibacterial.
A new series of N-acyl hydrazones (4a-g) derived from indole-3-propionic acid (IPA) were synthesized. These N-acyl hydrazones were prepared by the reaction of 3-(1H-indol-3-yl) propane hydrazide and aldehyde in the existence of glacial acetic acid as a catalyst. 1HNMR and FT-IR analyses were used to identify the synthesized compounds and they were in vitro evaluated as antibacterial agents against six different types of microorganisms by using well diffusion method. All the tested N-acyl hydrazones (4a-g) displayed moderate activity against the Gram-negative E.coli, comparable to that of Amoxicillin. Some of the tested N-acyl hydrazones also exhibited intermediate activity ag
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Publication Date
Sun Jun 09 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Preliminary Anti-inflammatory Evaluation of New Etodolac Derivatives
: Etodolac hydrazone derivatives
Anti-inflammatory
Paw edema method.
Three new hydrazone derivatives of Etodolac were synthesized and evaluated for their anti-inflammatory activity by using egg white induced paw edema method. All the synthesized target compounds were characterized by CHN- microanalysis, FT-IR spectroscopy, and 1HNMR analysis. The synthesis of the target (P1-P3) compounds was accomplished following multistep reaction procedures. The synthesized target compounds were found to be active in reducing paw edema thickness and their anti-inflammatory effect was comparable to that of the standard (Etodolac).
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Publication Date
Mon Dec 01 2008
Journal Name
Journal Of Economics And Administrative Sciences
السياسة النقدية في العراق بعد 9/4/2003 (الواقع والطموح)
السياسة النقدية في العراق بعد 9/4/2003 (الواقع والطموح)
لا يستطيع كل كائن حي أو كيان اجتماعي أداء دوره الذي يفترض أن يقوم به ما لم يمتلك الوسائل الكافية والضرورية لأداء ذلك الدور قال سبحانه وتعالى ((قال ربنا الذي أعطى كل شيء خلقه ثم هدى – طه 50)).
والنشاط الاقتصادي كجزء من الكيان الكلي للمجتمع لا يختلف عن هذه القاعدة، إذ عندما يراد من النظام الاقتصادي أداء دور فاعل فلا غنى له عن الوسائل التي تمكنه من أداء دوره المنشود. للنظام الاقتصادي مجمو
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Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of General Chemistry
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