Synthesis and Antibactrial Study of New  2-Amino-5-Aryl- 1,3-Thiazole-4-Carboxylic Acid Derivatives

Zina K. Al- Dulaimy; Aoras A. Kadhim; Abduljabbar Kh. Attia; Mohammed Z. Thani

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Publication Date

Wed Apr 26 2017

Journal Name

Ibn Al-haitham Journal For Pure And Applied Sciences

Volume

26

Issue Number

2

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Synthesis and Antibactrial Study of New 2-Amino-5-Aryl- 1,3-Thiazole-4-Carboxylic Acid Derivatives

1

3-thiazole-4-carboxylic acid

imide derivatives

Schiff's base.

Zina K. Al- Dulaimy

Aoras A. Kadhim

Abduljabbar Kh. Attia

Mohammed Z. Thani

...Show More Authors

2-Amino-5-aryl- 1,3-thiazole-4-carboxylic acid (A1-A3) were synthesized from the reaction of various aromatic aldehyde with dichloro acetic acid and thiourea. The synthesis of 2-[[(Saminosulfinim-idoyl)(aryl)methyl](benzoyl)amino]-5-aryl-1,3-thiazole-4-carboxylic acid (A22-A30) was perfomed starting from (A1-A3) by two steps using Schiff's base (A4-A12) prepared from the reactant compounds (A1-A3) with different aromatic aldehyde. Finally two types of imide derivatives were obtained from reactant compounds (A1-A3) with malic anhydride (A31-A33) and phthalic anhydride (A34-A36) in the presence of glacial acetic acid. All proposed structures were supported by FT-IR and UV-Visible spectroscopic data.

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Publication Date

Wed Mar 10 2021

Journal Name

Baghdad Science Journal

Synthesis & Characterization of Oxazinan and 5-oxa-7-aza-spiro[2,5] octane from reaction of Dibenzylidene with malonic anhydride and 5-oxa-spiro[2,3] hexane-4,6-dione.

Waleed, F.

Obaid H.

Mohammed A

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Di Benzylidenes were prepared by condensation of 1,2-diamino benzene with o- hydroxy benzaldehyde. These dibenzylidenes when treated with one equivalent of malonic anhydride or 5-oxo-spiro[2,3]hexane-4,6-dione in dry benzene give 6-membered heterocyclic ring system of 3-{2-[(2-Hydroxy-benzylidene)-amino]-phenyl}-2-(2-hydroxy –phenyl)-[1,3]oxazinane-4,6-diones ( 1-3) or 7-{2-[(2-hydroxy-benzylidene)-amino]-phenyl}-6-(2-hydroxy-phenyl)-5-oxa-7-aza-spiro[2.5]octane-4,8-diones ( 7- 9 ) But when two equivalents of malonic anhydride or 5-oxo-spiro[2,3]hexane-4,6-dione were used and under sam conditions compounds (4-6 , 10-12 ) were obtained .

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Publication Date

Thu Jun 21 2012

Journal Name

J Bagh Coll Dent

Dental caries in relation to oral infections and feeding types among children aged 2-5 years

Aseel Haidar M.J.

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Publication Date

Thu Jul 20 2023

Journal Name

Ibn Al-haitham Journal For Pure And Applied Sciences

Synthesis, Characterization and Biological Activity Study for Some New Metals Complexes with (3Z,3'E)-3,3'-(((2E,5E)-hexane-2,5-diylidene)bis(hydrazine-2,1-diylidene))bis(indolin-2-one)

antibiotic

FTIR

1H-NMR

Mass

Schiff-species

Hexadion

Isatin-3-hydrazone

Schiff_bases complexes

biological activity

Nuha Ayad

Naser Dheyaa

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Our recent work displays the successful preparation of Schiff_bases that carried out between hexane-2,5-dione and 2 moles of (Z)-3-hydrazineylideneindolin-2-one forming in Schiff-bases-(L), Which in turn allowed combining with each of the next metal ions: (M²⁺) = Ni, Mn, Zn, Cu and Co forming complexes_ in high stability. The formation of resulting Schiff_ bases (L) is detected spectrally using LC_Mss which gave approximately matching results with theoretical incomes, ¹HNMR proves the founding of doublet signal of (2H) for 2NH, FTIR indicates the occurrence of two interfered imine bands and UV-VIS mean is also indecates the formation of ligand. On the other hand, complexes-based-Schiff were characterized using the s

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Publication Date

Sat Jun 12 2021

Journal Name

Biochemical And Cellular Archives

EFFECT OF SINGLE ORAL DOSE OF FUMONISIN B1 ON IMMUNOHISTOCHEMICAL EXPRESSION OF TLR-2 AND 4 IN MICE

FB1

IHC

TLR-2 & 4

liver

kidney

Huda

Sinai W.

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Fumonisin B1 is toxic secondary metabolites compound produced by Fusarium spp. on maize and maize products causes health problems to human and animal. Therefore, this research is planned to study the effect of FB1 on the expression of TLR-2 & 4 in liver and kidney cells of mice. Four group of male mice were orally administrated with single dose of FB1 toxin as the following: 0 ppb, 800 ppb, 1200 ppb and 1600 ppb. After two weeks all animals were sacrificed, liver and kidney autopsies were taken and the level of TLR-2 & 4 detected in each four group by immunohistochemistry technique (IHC). According to the IHC examination of groups (1, 2, 3 and 4) strong expression of TLR2 in liver and kidney were (0%, 33.3%, 100%, 100%), respectively. This

Publication Date

Sat Sep 23 2017

Journal Name

Ibn Al-haitham Journal For Pure And Applied Sciences

Synthesis and Characterization of New ligand ' ((2-{1..,[(2-hyd_roxy;..benzyli_dene)-hydrazono]- ethyl} benzen_e-l, 3, s--moll and ItComplexes WÂ·itll. (Mn.(11 Fe(n), Cd<11J, a-nd Hg(n).) Tons

A .T.

M.

1\1.

...Show More Authors

In :the _pr sent _paper we report ths. ynthesis Â·of a new li:ga!!d..

[f4LJ [{'2 {1-'[(2-hydâ€¢:0xy-.ben:zy1i.denÂ·e)..,bxcJrazanci}:etby-l }benzerieÂ

J,5 t;rtiol .aad its complexes Â·w-ith '('Mlif(1 J Fev 1 ), ed(J'l), and. :f.::I:g 01>-)

The ligand \VS preP..ated rin tWo steps' â€¢ fp I t}Je nrst stea -soJutiQil Qf

-saUcyla[deeyeq. ip methatt:oJ . re3ctcd lU1der reflux

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Publication Date

Mon Aug 07 2017

Journal Name

Ibn Al-haitham Journal For Pure And Applied Sciences

The Inhibitory Effect of Some Benzoic Acid Derivatives on Human Erythrocyte Catalase Activity

Z.A.

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In order to study the kinetic of human erythrocytes catalase a well â€“known enzyme uses H2O2 as substrate as well as hydrogen acceptors, in non smokers and smoker individuals. Anthranilic acid and p-Amino Benzoic Acid (PABA) were used to study their effect on the enzyme. The kinetic study confirmed that anthranilic is a non-competitive inhibitor with Km values of 0.95 and 1.0 for non smokers and smokers respectively (PABA) was found to be a competitive inhibitor with Vmax values of 8.0 and 8.9 for nonsmoker and smoker respectively

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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.

Kinaan M

...Show More Authors

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Publication Date

Thu Aug 08 2024

Journal Name

New Materials, Compounds And Applications

MOLECULAR MODELLING AND THEORETICAL DESIGN OF NOVEL NIRMATRELVIR DERIVATIVES AS SARS-COV-2 ENTRY INHIBITORS

Mohammed

Wurood

...Show More Authors

The pandemic SARS-CoV-2 is highly transmittable with its proliferation among nations. This study aims to design and exploring the efficacy of novel nirmatrelvir derivatives as SARS entry inhibitors by adapting a molecular modeling approach combined with theoretical design. The study focuses on the preparation of these derivatives and understanding their effectiveness, with a special focus on their binding affinity to the S protein, which is pivotal for the virus’s access to the host cell. Considering molecular docking aspects in the scope of a study on nirmatrelvir derivatives and S protein, dynamics simulations with 25 nanoseconds of their binding are explored. The study shows that these derivatives might work as effective antivi

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Publication Date

Mon Apr 17 2017

Journal Name

Ibn Al-haitham Journal For Pure And Applied Sciences

Synthesis And Imidization Of Disuccinamic Acid As Polyvinyl Alcohol-Composite Polymer

Succinic anhydride

1

4-pheneylenediamin dihydrochloride

binzidine

acetic anhydride-sodium acetate

PVA

Zakaria H.

Fadhel S.

Hiba A. Ghani

...Show More Authors

Two arylenedisuccinamic acids, namely 1,4-phenylene-disuccinamic acid and 4,4'biphenyl-disuccinamic acid were prepared from the reaction of two moles of succinic anhydride with one mole of 1,4-phenylenediamine dihydrochloride and beinzidine respectively.Dehydration of arylenedisuccinamic acid in the pressence of polyvinyl alcohol (PVA) and catalytic amount of concentrated.H2SO4,gives N,N'-arylenedisuccinimidesPVAcomposite polymers. Dehydration of arylenedisuccinamic acid (without PVA) in the pressence of catalytic amount of conc. H2SO4 gives N,N'-arylenedisuccinimides. Arylenedisuccinamic acid and arylenedisuccinimides characterized by CHN-analysis,FT.IR and 1H,C13-NMR.Spectral analysis

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Publication Date

Fri Apr 01 2022

Journal Name

Baghdad Science Journal

Synthesis and Characterization of New Benzothiazole-derived Schiff Bases Metal Complexes

aniline

1

3-benzothiazole

ligand

metal complexes

Schiff bases

Wasan Abdul Razzaq

Areej Kamal Assim

Muhanned A.

...Show More Authors

Nitrogen-comprising heterocyclic compounds and their derivatives have empirically been invaluable as therapeutic agents. Fundamentally, 4-chloro-6-nitro-2-amino-1,3-benzothiazole 1 was synthesized via bromination of 2-chloro-4-nitro aniline with ammonium thiocyanate. This new heterocyclic haloorganoamino-1,3-benzothiazole derivative, was a starting material, which condensed and tethered with three different aromatic aldehyde pendant arm in presence of ethanol and glacial acetic acid isolating an interesting sequence of tridentate Schiff bases 2-4. These compounds were used for complexation reactions in 1:1 (metal: ligand) stoichiometry to obtain heteroleptic Al(III), Ni (II) and K(I) benzothiazole chelat

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