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bsj-7402
Synthesis, Anticancer and Antibacterial Activity of Mannose-based bis-1,2,3-Triazole Derivatives
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       In the current work, aromatic amines and alkyl halides have been converted to the corresponding azides 2a‒d and 4a-d by the reaction with sodium nitrite and sodium azide respectively for amines and sodium azide for halides. Then, dipropargyl ether derivative of D-mannose 8 has been synthesized from diacetone mannose that has been obtained by the treatment of D-mannose (5) with dry acetone in the presence of sulfuric acid. Then, aldol condensation has been used to prepare diol 7 from the mannose diacetonide 6. The reaction of compound 7 with propargyl bromide in alkaline media has been afforded dipropargyl derivative 8. In a parallel step, both dialkyne with aromatic and aliphatic azide have been coupled to produce 1,2,3-triazole derivatives 9ad in the presence of Cu(I) salts. All synthesized compounds have been characterized by 1D and 2D NMR spectra alongside with HRMS data. The antibacterial activity against both gram-positive and gram-negative has been tested. Moreover, the anticancer activity has also been evaluated against AMJ13 cell line.

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of Coumarin Derivatives Coupled to Amino Acid Esters and Studying their Biological Activity as Antimicrobial Agents
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A series of coumarin derivatives linked to amino acid ester side chains were synthesized and evaluated of their antibacterial and antifungal activity. The coumarin derivatives was alkylated by the ethyl bromoacetate and then using potassium carbonate to get alkylated hymecromone. Conventional solution method for amide bond formation was used as a coupling method between the carboxy-protected amino acids with acetic acid side chain of coumarin derivatives. The DCC/ HOBt coupling reagents were used for peptide bond formation. The proposed analogues were successfully synthesized and their structural formulas were consistent with the proposed struct

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis, Characterization and Antibacterial Activity of New Chalcones Derived from New Aldehyde; 4-[5-(4`tolyl)-1,3,4-thiadiazole-2-yl] benzaldehyde
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 New chalcones of  -{ -  -   -   y  -     - hi di z  e- -y    he y  - -    e e- -  e-    -        - substituted phenyl have been prepared from condensation of  a new of  4-[5-(4`-tolyl)1,3,4-thiadiazole-2-yl] benzaldehyde (which is synthesized by the reaction of  2- amino-5- (4`-tolyl) -1,3,4-thiadiazole and benzaldehyde) with 3- or 4- substituted acetophenones in alkaline medium. The physical, CHNS analysis and spectral data of the synthesized compounds were determined. The biological activity evaluated of new compounds showed that many of these compounds possess antiba

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Publication Date
Wed Jan 01 2020
Journal Name
Research Journal Of Pharmacy And Technology
<i>Insilico</i> and <i>in vitro</i> Approach for Design, Synthesis, and Anti-proliferative Activity of Novel Derivatives of 5-(4-Aminophenyl)-4-Substituted Phenyl-2, 4-Dihydro-3<i>H</i>-1, 2, 4-Triazole-3-Thione
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Publication Date
Sun May 14 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Antibacterial Activity of Calendula Officinalis Flowers In Vitro
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        Flower  samples of Calendula officinalis were collected from the gardens of the college of Pharmacy in Baghdad city  to examine their antibacterial activity .The effect of ethanol crude extract of petals and reproductive parts of flowers in different concentrations were obtained and bioassayed in vitro for its bioactivity to inhibit the growth of eight types of bacteria .The extracts of petals  part were clearly superior for all bacteria especially the bacteria Pseudomonas aeruginosa (inhibition zone was 25mm in the concentration 100mg/ml) from gram negative bacteria, and Staphylococcus aureus (inhibition zone was 14mm in the concentration 50mg/ml) from gram positive bacteria, whi

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Publication Date
Wed Jan 01 2020
Journal Name
Systematic Reviews In Pharmacy
Synthesis of New Ibuprofen Derivatives Containing (Oxothiazolidin-3-yl) Amino Moiety with Expected Biological Activity
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Nonsteroidal anti-inflammatory drugs (NSAIDs) are drugs that help reduce inflammation, which often helps to relieve pain. In this research new ibuprofen oxothiazolidnone derivatives were synthesized from the reaction of Schiff base derivatives of Ibuprofen with mercapto acetic acid VI a-c, to improve the potency and to decrease the drug's potential side effects, a new series of 4-thiazolidinone derivatives of ibuprofen was synthesized VI a-c . The characterizations of the compounds were identified by using FTIR, 1HNMR technique and by measuring the physical properties.

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Publication Date
Sat Dec 21 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Preliminary Anticancer Study of Novel 5-fluorouracil Conjugate with Pyrrolidine Dithiocarbamate as a Mutual Anticancer Prodrug
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 5-Fluorouracil is one of the commonly used chemotherapy drugs in anticancer therapy; unfortunately treatment with 5-FU by solely has many drawbacks  low lipophilicity, low permeability, low molecular weight, and its relatively poor plasma protein binding; also a brief half-life therefore frequent administration is required to maintain the optimal therapeutic plasma level which in addition to its poor selectivity, drug resistance and limited penetration to cancer cells; leads to increased incidence of side-effects to healthy cells/tissues and low response rates. In order to minimize these drawbacks; 5-FU was chemically  conjugated with pyrrolidine dithiocarbamate (PDTC) in a mutual prodrug moiety (S-(9H-purin-6-yl) 3-(

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Publication Date
Sun Jun 09 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
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Small molecules drug conjugate mutual prodrug design  (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide  bond   ;  represent new interesting approaches for cancer treatment , the component of SMDC intended  for targeting    folate receptor , along with greater conservation  of component until reaching  the target tumor tissue . The  designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were  processed forward  successfully by multistep reaction  procedures , and by Thin Layer Chromatography (TLC) for

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Publication Date
Sat Feb 02 2019
Journal Name
Journal Of The College Of Education For Women
The art of patchwork in designing and making night gowns and their supplements: The art of patchwork in designing and making night gowns and their supplements
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Abstract:
If we neglect the value of historical fashions as a source of inspiration for
contemporary fashion designers we will neglect a treasure of original designs.
In neglecting such a treasure how could we then know what is original. Today
the most famous fashion designers are often inspired, in the outwardly from
and internal lines of their fashions, by fashion designed during the ages of the
past.
Designers can find such fashions in books of history and museums. But
the historical ages are not equal in the fertility of the originality and novelty of
their fashions. Thus the contemporary designer may not find the old designs
inspiring so he invents them.
The researcher was keen in this paper to inclu

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Publication Date
Wed Jun 01 2022
Journal Name
Baghdad Science Journal
Syntheses, Structures and Biological Activity of Some Schiff Base Metal Complexes
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Four new binuclear Schiff base metal complexes [(MCl2)2L] {M = Fe 1, Co 2, Cu 3, Sn 4, L = N,N’-1,4-Phenylenebis (methanylylidene) bis (ethane-1,2-diamine)} have been synthesized using direct reaction between proligand (L) and the corresponding metal chloride (FeCl2, CoCl2, CuCl2 and SnCl2). The structures of the complexes have been conclusively determined by a set of spectroscopic techniques (FT-IR, 1H-NMR, and mass spectra). Finally, the biological properties of the complexes have been investigated with a comparative approach against different species of bacteria (E. coli G-, Pseudomonas G-, Bacillus G+,

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Publication Date
Wed Mar 25 2020
Journal Name
Biomedical And Pharmacology Journal
Synergistic Antibacterial Activity of Epidermin and Staphylolysin LasA against Pathogenic Bacteria
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Antibiotic resistance increment is a major problem for the human society nowadays which encourages the efforts to look for new therapeutic alternatives from natural defenses. Synergistic antibacterial activity of epidermin and staphylolysin LasA A against Staphylococcus aureus (Staph aureus), Escherichia coli (E. coli) and Pseudomonas aeruginosa (Ps. aeruginosa) was evaluated. The antibacterial activities of epidermin from Staphylococcus epidermidis (Staph epidermidis) and Staphylolysin (LasA) from Ps. aeruginosa using the agar well diffusion assay were evaluated, and then using the micro dilution method to evaluate the minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC). The checkerboard method and fract

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