Preferred Language
Articles
/
bijps-531
Synthesis and Preliminary Pharmacological Study of Sulfonamide Conjugates with Ibuprofen and Indomethacin as New Anti-Inflammatory Agents
...Show More Authors

          4-aminobenzenesulfonamide conjugates of ibuprofen (compound 10) and indomethacin (compound 11) have been designed and synthesized by the reaction of sulfanilamide (compound 7) with 2-(4-isobutylphenyl) propanoic acid (ibuprofen) and 2-(1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl)acetic acid (indomethacin) for the evaluation as potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the synthesized final compounds (10 and 11) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (10mg/Kg) of ibuprofen and (2mg/kg) of indomethacin. The tested compounds produced significant reduction of the rat paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compound (10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) (reference group) while compound (11) exhibited less anti-inflammatory activity than diclofenac. The result of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore into ibuprofen and indomethacin maintained their anti-inflammatory activity & may increase their selectivity toward COX-2 enzyme which can be confirmed in future by assessing COX-2:COX-1 inhibitory ratio.

Key words: Cyclooxygenase; Anti-inflammatory activity; Ibuprofen; indomethacin; NSAIDs.

Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Mon Jan 01 2024
Journal Name
Vitae
Enzyme Inhibitory and Anti-cancer Properties of Moringa peregrina
...Show More Authors

Background: Moringa peregrina is widely used in the traditional medicine of the Arabian Peninsula to treat various ailments, because it has many pharmacologically active components with several therapeutic effects. Objective: This study aimed to investigate the inhibitory effect of Moringa peregrina seed ethanolic extract (MPSE) against key enzymes involved in human pathologies, such as angiogenesis (thymidine phosphorylase), diabetes (α-glucosidase), and idiopathic intracranial hypertension (carbonic anhydrase). In addition, the anticancer properties were tested against the SH-SY5Y(human neuroblastoma). Results: MPSE extract significantly inhibited α-glucosidase, thymidine phosphorylase, and carbonic anhydrase with half-maximal i

... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Sun Dec 04 2011
Journal Name
Baghdad Science Journal
Preparation and Spectral Study of New Complexes of Some Metal Ions with 3,5-Dimethyl-1H-Pyrazol-1-yl Phenyl Methanone
...Show More Authors

Many complexes of 3,5-dimethyl-1H-pyrazol-1-yl phenyl methanone with Cr(III), Co(II), Ni(II), Cu(II) and Cd(II) were synthesized and characterized by FT-IR, UV/visible spectra, elemental analysis, room temperature magnetic susceptibility and molar conductivity. Cd(II) complex was expected to have tetrahedral structure while all the other complexes were expected to have an octahedral structure.

View Publication Preview PDF
Crossref
Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis and Evaluation Antibacterial Activity of Some New Substituted 5-Bromoisatin Containing Five, Six Heterocyclic Ring
...Show More Authors

This research includes the synthesis of some new different heterocyclic derivatives of 5-Bromoisatin. New sulfonylamide, diazine, oxazole, thiazole and 1,2,3-triazole derivatives of 5-Bromoisatin have been synthesized. The synthesis process started by the reaction of 5-Bromoisatin with different reagents to obtain schiff bases of 5-Bromoisatin intermediate compounds(1, 8, 19) by using glacial acetic acid as a catalyst in three routes. The first route, 5-Bromoisatin reacted with p-aminosulfonylchloride to product compound(1), then converted to sulfonyl amide derivatives(2-7) by the reaction of compound(1) with different substituted primary aromatic amine in absolute ethanol. The second route includes the reaction of 5-Bromoisatin rea

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Sun Sep 22 2019
Journal Name
International Journal Of Pharmaceutical Research
Synthesis, Characterization and Antibacterial of Some New 4,4'-(pyridine-2,6-diylbis(1,3,4- oxadiazole-5,2-diyl))bisphenolPolymer
...Show More Authors

4,4'-(pyridine-2,6-diylbis(1,3,4-oxadiazole-5,2-diyl))bisphenol monomer (3)was synthesized from cyclization of N'2,N'6-bis(4-hydroxybenzylidene)pyridine-2,6-dicarbohydrazide (2)in the presence of bromine in glacialacetic acid. Newly five polymers (P1-P5) were synthesized from reaction bis-1,3,4-oxadiazole bisphenolmonomer with five different di acid chloride. The antibacterial activity of the synthesized polymers was screened against gram positive and gram negative bacteria. Polymers P4 and P5 exhibited significant antibacterial against all microorganisms, as well these polymers showed highest antifungal activity.

Publication Date
Wed Jul 28 2021
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization, and Biological Studies of New Complexes Derived from 2-(1H-Benzimidazol-2-yl) Aniline
...Show More Authors

The Schiff base (E)-2-(((2-(1H-benzo[d]imidazol-2-yl) phenyl) imino) methyl)-4-methylphenol (Lb) ligand with some metals(II) ion such as; Co, Cu, Cd, and Hg, were synthesis and characterized by the mass and 1 HNMR spectrometry for ligand Schiff base, the fourier-transform infrared spectroscop (FTIR), UV- visible and the flame atomic absorption (AA) spectrum, the CHN analysis, and the chlorine content, in addition to measuring the magnetic sensitivity of the complexes. All the complexes had octahedral geometry. The bioactivity activity for compounds against; Rhizopodium, Staphylococcus aureus, and Escherichia coli showed different efficacy towards these microorganisms

Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Pharmacy Research
Synthesis and antimicrobial evaluation of new-[2-amino-4- (4-chloro-/4-bromophenyl)-1,3-thiazole derivatives
...Show More Authors

Publication Date
Thu Feb 02 2023
Journal Name
Aip Conference Proceedings
Designed new mesogence containing 5Hthiazolo[3,4-b][1,3,4]ihiadiazole: Synthesis and investigation of liquid crystals properties
...Show More Authors

This research include synthesized and characterization the compound [I] by reaction terephthaldehyde , mercaptoacetic acid and thiosemicarbazide with concentrated sulfuric acid then this compound reaction with ethyl chloroacetate and sodium acetate to product ester compound [II],the latter compound reaction with hydrazine hydrate to synthesized acid hydrazide [III] after that reaction with 4-alkoxy benzaldehyde[IV]n to synthesized Schiff bases compounds [V]n, the compound [VI] synthesized via reaction compound [I] with chloroacetic acid and sodium acetate then the compound[VI] reaction with 2-phenylenediamine in 4 N hydrochloric acid to product benzimidazole compound[VII]. The compounds characterized by melting points, FTIR and 1HNMR spectr

... Show More
Preview PDF
Publication Date
Mon May 15 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of New Schiff Bases and 2,3-Disubstituted 1,3-Thiazolidin-4-one Derivatives Containing Benzothiazole Moiety
...Show More Authors

  Two series of Schiff Bases and 2,3-disubstituted-1,3-thiazolidin-4-one derivatives  were synthesized . Reaction of 2-mercaptobenzothiazole with α-chloro acetic acid gave compound[I]. Esterification of carboxylic moity of compound [I] , using absolute methanol in the presence of conc . H2SO4 yielded acorresebonding ester  [II] , wich was condensation with hydrazine hydrate to give acid hydrazide [III] . The new Schiff bases [V]n were synthesized by reaction of acid hydrizide with dialdehyde [IV]n  in the presence of glacial acetic acid . The thiazolidinone derivatives [VI]n  have been obtained from the azomethines through the addition of thioglycolic acid . Their chemical structures have been confirmed by mel

... Show More
View Publication Preview PDF
Publication Date
Mon Jun 01 2009
Journal Name
Engineering And Technology Journal
Synthesis and study of the Novel tetradented ligand type N2O2 and its complexes with (Mn (II) ,Co (II) ,Ni (II) and Cu(II)) ions
...Show More Authors

A new Schiff base ligand Bis-1,4-di[N-3-(2-hydroxy-1-amino)- acetophenonylidene] benzylidene [L] and its complexes with (Mn(II) ,Co(II) ,Ni(II and Cu(II)) were synthesized . The ligand was prepared in two steps. In the first step a solution of (terphthalaldehyde) in methanol reacts under reflux with (p-aminoacetophenone) to give an intermediate compound [1-[3-({4-[(3-Acetyl-phenylimino)-methyl]-benzylidene}-amino)-phenyl]- ethanone which reacts in the second step with (2-Amino-phenol) giving the mentioned ligand. The complexes were synthesized by addition the corresponding metal salt solution to the solution of the ligand in methanol under reflux in (1:1) metal to ligand ratio. On the basis of, molar conductance, I.R., UV-Vis, HPLC, chlorid

... Show More
Publication Date
Mon Feb 20 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New 2-thioxoimidazolidin-4-one Derivatives
...Show More Authors

This research includes the synthesis of new series of heterocyclic compounds. Reaction of 2-nitro benzylidene)thiosemicarbazide(1) with ethyl chloro acetate gave (2-nitro benzylidene amino)-2-thioxomidazolidine-4-one(2) ,treatment(2) with methyl iodide to give(3)which was reacted with hydrazine to give 2-hydrazinyl-1-[(2-nitrobenzylidene)amino]- 1H-imidazol-5(4H)-one, andreation of compound(2) with aromatic aldehydes to give 5arylidene -3-({2-nitro benzylidene}amino)2-thioxo-3,5-dihydro-4H-imidazole-4-one(5a,5b), which was reacted with ethyl aceto acetate to give 4-aryl-1-[2-nitrobenzylidene, amino -6oxo-2-thioxo octa hydro-1H-benzo[d]imidazole-5-carboxylate and followed synthesis of βlactamederivtives(9a,9b) by treatment derivatives(

... Show More
View Publication Preview PDF