Synthesis and Study of the Biological Activity of New Compounds Derived from 4-(5-Phenyl-1,3,4-oxadiazole-2-yl)aniline
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Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Isatin-Ibuprofen Derivatives with Expected Biological Activity
Ibuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard
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Publication Date
Sun Dec 25 2022
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization of New Isatin-Ibuprofen Derivatives with Expected Biological Activity
Biological activity
Ibuprofen
Isatin
5- Methoxy isatin
Ibuprofen is one of the most important members of NSAIDs, named aryl propionic acid derivative. Isatin (1H-indole-2,3-dione) is an important molecule of heterocyclic compounds that have many biological activities. This work illustrates the synthesis of new ibuprofen-isatin derivatives by connecting ibuprofen hydrazide with different isatin derivatives by a condensation reaction, followed by characterization by fourier-transform infrared spectroscopy (FTIR) and proton nuclear magnetic resonance (1H-NMR) spectroscopy. The anti-inflammatory activity was evaluated by using the egg-white induce edema method for all the synthesized compounds (5-8), the compounds 5 and 6 showed better anti-inflammatory activity than ibuprofen as a standard compoun
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Publication Date
Mon Apr 01 2019
Journal Name
Journal Of Pharmaceutical Sciences And Research
Publication Date
Thu Oct 08 2015
Journal Name
Journal Of Kerbala University
Synthesis, Spectroscopic and Biological Studies of some metal ions complexes with 1-Phenyl-3-pyridin-2-ylmethyl-thiourea
حضر الليكاند (L) 1-فنيل-3-بردين-2-يل مثيل-ثايويوريا من تفاعل 2-أمينو مثيل بردين مع فنيل ايزوثايوسيانيت وبنسبة 1: 1 وشخص الليكاند بواسطة التحليل الدقيق للعناصر (C, H, N), الأشعة تحت الحمراء، الأشعة فوق البنفسجية–المرئية وطيف الرنين النووي المغناطيسي كما حضرت وشخصت معقدات أملاح بعض ايونات العناصر الثنائية التكافؤ (Co, Ni, Cu, Cd and Hg). استخدمت تقنية الأشعة تحت الحمراء، الأشعه فوق البنفسجية-المرئية, التوصيلية الكهربائية و الا
... Show MorePublication Date
Thu Sep 16 2010
Journal Name
Al-mustansiriyah
Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis and Characterization of New Phthalimides Containing 1, 2, 4-triazole and Imine Group
Several new derivatives of 1, 2, 4-triazoles linked to phthalimide moiety were synthesized through following multisteps. The first step involved preparation of 2, 2-diphthalimidyl ethanoic acid [2] via reaction of two moles of phthalimide with dichloroacetic acid. Treatment of the resulted imide with ethanol in the second step afforded 2, 2-diphthalimidyl ester [3] which inturn was introduced in reaction with hydrazine hydrate in the third step, producing the corresponding hydrazide derivative [4]. The synthesized hydazide was introduced in different synthetic paths including treatment with carbon disulfide in alkaline solution then with hydrazine hydrate to afford the new 1, 2, 4-triazole [10]. Reaction of compound [10] with different alde
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Fri Aug 25 2017
Journal Name
Oriental Journal Of Chemistry
Relationship Between the structure of Newly Synthesized derivatives of 1,3,4-oxadiazole Containing 2-Methylphenol and their Antioxidant and Antibacterial Activities
2-methylphenol
hindered phenol
1
3
4-oxadiazole
antioxidant
antibacterial
1,3,4-oxadiazole-5-thion ring (2) successfully formed at position six of 2-methylphenol and five of their thioalkyl (3a-e). Furthermore 6-(5-(Aryl)-1,3,4-oxadiazol-2-yl)-2-methylphenol (5a-i) were formed at position six by two method. The first method was from cyclization their corresponding hydrazones (4a-e) of 2-hydroxy-3-methylbenzohydrazide (1) using bromine in glacial acetic acid. The second method was from cyclization the hydrazide with aryl carboxylic acid in the presence of phosphorusoxy chloride. The newly synthesized compounds were characterized from their IR, NMR and mass spectra. The antioxidant properties of these compounds were screened by 2,2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) assay
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Publication Date
Fri Aug 25 2017
Journal Name
Oriental Journal Of Chemistry
Relationship Between the structure of Newly Synthesized derivatives of 1,3,4-oxadiazole Containing 2-Methylphenol and their Antioxidant and Antibacterial Activities
2-methylphenol
hindered phenol
1
3
4-oxadiazole
antioxidant
antibacterial
1, 3, 4-oxadiazole-5-thion ring (2) successfully formed at position six of 2-methylphenol and five of their thioalkyl (3a-e). Furthermore 6-(5-(Aryl)-1, 3, 4-oxadiazol-2-yl)-2-methylphenol (5a-i) were formed at position six by two method. The first method was from cyclization their correspondinghydrazones (4a-e) of 2-hydroxy-3-methylbenzohydrazide (1) using bromine in glacial acetic acid. The second method was from cyclization the hydrazide with aryl carboxylic acid in the presence of phosphorusoxy chloride. The newly synthesized compounds were characterized from their IR, NMR and mass spectra. The antioxidant properties of these compounds were screened by 2, 2-Diphenyl-1-picrylhydrazide (DPPH) and ferric reducing antioxidant power (FRAP) a
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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
Mon Mar 27 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of New B-adrenoceptor Blocking Agent Including 1,3,4 Thiadiazole with Expected Adrenoceptor Blocking Activity
β-Adrenergic blocking agents, mostly comprising of β-amino alcohols, are of pharmaceutical significance and have received major attention due to their utility in the management of cardiovascular disorders including hypertension, angina pectoris, cardiac arrhythmias and other disorders related to the sympathetic nervous system. Most compounds available for clinical use belong to the aryloxypropanolamine series, which is considered the second generation of β-blocking agents. The present study includes the synthesis of compounds with an N-substituted oxypropanolamine moiety attached to the 1, 3, 4-thiadiazole derivatives. According to this information, eight compounds were synthesized and characterized by IR spectra and elemental m
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