Preferred Language
Articles
/
VheymZIBVTCNdQwCWrmQ
Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
...Show More Authors

Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds were synthesized and characterized by successfully by ART-FTIR, NMR and ESI- Ms. Assessed for their cytotoxic activity against human colon adenocarcinoma MCF-7 (IC50, I=105.15, II=60.00, III=54.11, IV=56.57, vorinostat=28.41) and hepatoblastoma HepG2 (IC50, I=63.91, II=135.18, III=118.85, IV=51.46, vorinostat=37.50). Most of them exhibited potent HDAC inhibitory activity and significant cytotoxicity. Conclusions: The synthesized compounds (I, II, III and IV) showed cytotoxicity toward MCF-7 and HepG2 cancer cell lines and their docking analysis provided a preliminary indication that they are viable [HDAC6] candidates.

Scopus Crossref
View Publication
Publication Date
Wed Apr 26 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Antibactrial Study of New 2-Amino-5-Aryl- 1,3-Thiazole-4-Carboxylic Acid Derivatives
...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.  
 

View Publication Preview PDF
Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Synthesis ,spectroscopic study of Antipyryl azo 2-Naphthol and use it as new reagent for determination of Co(II) and Cu(II)
...Show More Authors

A simple ,accurate and sensitive spectrophotometric method has been developed the determination of Cobalt(II) and Cupper (II) .The method is based on the chelation of Co(II) and Cu(II) ions with 4-(4´-pyrazolon azo) -2-Naphthol(APAN) in aqueous medium . The complexes have a maximum absorption at (513) and (506) nm and ? max 0.531×10 4 and 0.12×10 5 L.mol -1.cm -1 for Co(II) and Cu(II) respectively .The reagent and two complexes have been prepared in ethanolic solution.The stoichiometry of both complexes were found to be 1:2 (metal :legend) .The effects of various cations and anions on Co(II) and Cu(II) determination have been investigated .The stability constants and standard deviations for Co(II) and Cu(II) 0.291 x107 ,0.909X108 L.mol

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Jun 05 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Alpha Glucosidase Inhibition activity of new Phthalimide Derivatives
...Show More Authors

 Three of imide intermediate products  were synthesized by reacting of phthalic anhydride with glycine (2a), and tetrachloro phthalic anhydride with glycine , (S)-2-[(tert-Butoxycarbonyl)amino]-3-aminopropionic acid ( 2b,c)  respectively   in  dry toluene  with azeotropic removal of water using Dean- stark apparatus then carboxyl functional group activated by refluxing with  thionyl chloride, the resulted acid chloride (3a-c) were reacted with different amine (5-flourouracil, 4-chloroaniline, 4-bromoaniline, 2-amino thiazole, and pyrrolidine) (4a-e) , the   resulted products consider as

... Show More
View Publication Preview PDF
Scopus (4)
Crossref (2)
Scopus Crossref
Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and characterization of some new thiazolidinone derivatives containing indole ring
...Show More Authors

Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII] a, b and [VIII] a, b synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII] a, b,[VIII] a, b) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX] a, b and [X] ad). Finally, the new derivatives [XI] ac run out via the reacted compound [IX] a with different n-alkyl bromide (methyl bromide, ethyl bromide, and butyl bromide)

Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New heterocyclic Polyacrylamides from Derivatives 2-Aminobenzothiazole
...Show More Authors

The present work involved preparation of new hetro cyclic polyacrylamides (1-9) using reaction of polyacryloyl chloride with 2-aminobenzothiazole which prepeard by thiocyanogen method in the presence of a suitable solvent and amount tri ethyl amine (Et3N) with heating. The structure confirmation of polymers were proved using FT-IR,1H-NMR,C13NMR and UV spectroscopy.Other physical properties including softening and melting points, and solubility of the polymers were also measured.

View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Mon Mar 01 2021
Journal Name
Journal Of Physics: Conference Series
Synthesis and characterization of some new thiazolidinone derivatives containing indole ring
...Show More Authors
Abstract<p>Many new heterocyclic compounds including 4-thiazolidinones containing indole with triazole units were described. The new Schiff bases [VII]<sub>a, b</sub> and [VIII]<sub>a,b</sub> synthesized by condensation acid hydrazides [II],[VI] with different (aromatic) aldehydes in absolute ethanol. The refluxing equimolar amounts of the Schiff bases ([VII]<sub>a,b</sub>, [VIII]<sub>a,b</sub>) with thioglycolic acid in benzene led to get thiazolidin-4-ones derivatives ([IX]<sub>a,b</sub> and [X]<sub>a-d</sub>). Finally, the new derivatives [XI]<sub>a-c</sub> run out via the reacted compound [IX]<sub>a</sub> with di</p> ... Show More
View Publication
Scopus (1)
Crossref (2)
Scopus Crossref
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
Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis of Some New Heterocyclic Compounds Via Chalcone Derivatives
...Show More Authors

  The chalcones 1( a,b) were prepared by the reaction of  2- acetyl benzofuran with two aromatic aldehydes in the presence of alkaline media. These chalcones are used as starting material to obtain the  desired heterocyclic: pyrazolin, isoxazoline, pyrimidinthion, pyrimidinone, cyclohexanone and indazole derivatives. The structure of newly synthesized heterocyclic compounds were established on the basis of  their melting points, elemental analysis(C.H.N), FTIR and 1HMNR (for some of them) spectral data . The synthesized compounds have been screened for their antibacterial activities, they exhibited good antibacterial activity against Escherichia coli (G-) and Staphylococus aureus (G+) . 

View Publication Preview PDF
Publication Date
Sun Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring
...Show More Authors

In this work 5-methylene-yl - (2-methy –oxazole-4-one) (1H) imidazole (1) were synthesized from the reaction of L-Histidine with acetic anhydride and which converted to the of 5-methylene-yl-(2-methyl 3-amino imidazole-4-one)-1H-imidazole (2) by reaction with hydrazine hydrate. Schiff bases (3-6) were synthesized from the reaction of compound (2) with different aromatic aldehyde. Reaction of compounds (3-6) with chloroacetyl chloride gives azetidinone one derivatives (7-10). These compounds were characterized by FT-IR and some of them with 1H-NMR and 13C-NMR spectroscopy.

View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Thu Dec 29 2016
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of New Symmetrical Pyromellitdiimide Derivatives and Their Amic Acids
...Show More Authors

               The new symmetry pyromellitdiimide [VII]a-c,n  were synthesized by two-step reactions from the corresponding pyromellitic dianhydride . A new symmetrical amic acid [VI]a-c,n was synthesized by the reaction of pyromellitic dianhydride with different heterocyclic amines in dry acetone . The second reaction step includes  intramolecular cyclization of amic acid in the presence of  sodium acetate -acetic anhydride system at 850C. Structures  of  the synthesized compounds have been ascertained by their melting points , C.H.N analysis , UV-Vis, FTIR and 1HNMR spectroscopy.

View Publication Preview PDF