Preferred Language
Articles
/
bijps-489
Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
...Show More Authors

         A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds  produced a significant reduction  in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.                                                                                                                             

Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity.                                                                                                 

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Wed Jul 01 2020
Journal Name
International Journal Of Pharmaceutical Research
Synthesis and identification of some new N-substituted quinazoline-4-one, thiazine-4-one and tetrazoline rings incorporating N-ethyl-2-(benzylthio)benzimidazole acetate and study their application as anti-oxidant agent
...Show More Authors

View Publication
Scopus (2)
Crossref (1)
Scopus Crossref
Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents
...Show More Authors

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

Crossref (3)
Crossref
Publication Date
Thu Aug 20 2020
Journal Name
Al-mustansiriyah Journal Of Science
The Importance of 2-AminoThiazole Schiff Bases as Antimicrobial and Anticancer Agents
...Show More Authors

The pharmacophore 2-aminothiazole has an interesting role in pharmaceutical chemistry as this led to the synthesis of many types of compounds with diverse biological activity. Schiff base derivatives at the same time contribute to drug evolution importantly. In this review, the Schiff base derivatives of 2-aminothiazole formed and some of their metal complexes are being focused on, and the antimicrobial and anticancer activity of them is being illustrated.

View Publication
Crossref (3)
Crossref
Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Dose Dependent Anti-inflammatory Effect of Ammi majus Alcoholic Extract in Rat: Chronic Study
...Show More Authors

During treatment of inflammatory diseases, many conventional therapies (non-steroidal anti-inflammatory drugs) used to relief pain and inflammation. Chronic use of  the intended drugs is frequently associated with serious side effect, which may lead to discontinuation of treatment . The efficacy and dose- response effect of ammi majus extraxt  (2 , 4, 8 , 16, and 32 mg/rat) were assessed using  formalin to induce paw edema in rats as a model of chronic inflammation respectively. In this study,  42 rats were used and allocated into 7  groups each containing 6 rats, representing control (Distilled  water) , standard (piroxicam ) and test extract ( 2 , 4 , 8 , 16 and 32 mg/rat of Ammi majus alcoholic e

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Wed Jan 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Synthesis of anti-corrosion polymers from thiadiazole
...Show More Authors
Abstract<p>One of the biggest problems facing many industries particularly oil, is the problem of corrosion, where the metal parts under the influence of the vital factors are eroded during use and storage, therefore, to lift the metal’s ability and to protect it against corrosion, corrosion inhibitors are used. For the first time in this research, polymers which contain sulfur - heterocyclic ring with a thiadiazole base were made. Anti- corrosion polymers were made on two stages, in the first stage, thiadiazole was made from hydrazine hydrate reaction to carbon disulfide, afterwards the first product was reacted with an excess of hydrazine. In the second stage, polymers were prepared by the r</p> ... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Sat Jan 01 2022
Journal Name
Pharmacia
Synthesis, docking study, and structureactivity relationship of novel niflumic acid derivatives acting as anticancer agents by inhibiting VEGFR or EGFR tyrosine kinase activities
...Show More Authors

Scopus (24)
Scopus
Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization and Biological Evaluation of New Dithiocarbamate Ligand and Its Complexes with some Metal Ions
...Show More Authors

New bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil

... Show More
Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
...Show More Authors

The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

... Show More
Scopus (19)
Scopus
Publication Date
Fri Jan 01 2016
Journal Name
Der Pharmacia Lettre
Synthesis, characterization and anticonvulsant evaluation of new derivatives derived from 5-methoxy-2-mercapto benzimidazole
...Show More Authors

A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f

... Show More
View Publication Preview PDF
Scopus (4)
Scopus
Publication Date
Sat Jul 01 2023
Journal Name
Journal Of Nanostructures
Synthesis and Evaluation Biological Activity of Some New Polymers Derived From 3,3’-dimethoxybiphenyl-4,4’-diamine
...Show More Authors

In this study, synthesis of polymer Nanocomposites through the blending of prepared polymers with polyvinyl alcohol (a synthetic polymer) or chitosan (a natural polymer) then mixed with nano oxide silica by many steps. The new compound [I] was obtained via reaction of 3,3’-dimethoxybiphenyl-4,4’-diamine as starting material with malic anhydride in DMF then treatment with ammonium persulfate (NH4 )2 S2 O8 (as the initiator) in order to produce polymer [II]. Also, we prepared new polymers [III-V] by using the same starting material (3,3’-dimethoxybiphenyl-4,4’-diamine) with glutaric acid or adipic acid or isophthalic acid in DMF and pyridine. In this study, new polymer blending [VI-IX] and [X-XIII] were synthesized from a prepared pol

... Show More
View Publication
Scopus (3)
Scopus