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bijps-382
Design, Synthesis and Preliminary Antimicrobial Evaluation of New Derivatives of Cephalexin
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There is a continuous and massive need for newer cephalosporins that should have resistance against β-lactamases and can be used orally. An approach of using cephalexin, as a well-studied and potent antibacterial compound is considered to prepare new designed derivatives.  These derivatives include the incorporation of amino acid moiety linked through an amide bond with the α-amino group of cephalexin. Certain aliphatic amino acids were used, such as glycine, alanine, valine and proline. The chemical structures of these derivatives were confirmed by IR spectroscopy and elemental analyses. All the synthesized compounds were subjected for preliminary evaluation of antimicrobial activity using well diffusion method, against certain microbes. Most of the synthesized compounds were found to possess significant antibacterial activities.  Compound 1 (125 μg and 250μg) showed significant activity against P. aeruginosa. Compound 2 (125 and 250μg) exhibited significant activity against P. aeruginosa and Bacillus cereus.  Compound 3 (125 and 250μg) demonstrated very significant activity against E. coli, P. aeruginosa and Bacillus cereus and slight activity towards S. aureus. Compound 4 (250μg) showed significant activity against P. aeruginosa and no antibacterial activities against E. coli, S. aureus and Bacillus cereus, as compared with cephalexin as the standard compound.

Keywords: Cephalosporins, Cephalexin, Glycine, Alanine, Valine, Proline. 

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Publication Date
Mon Jul 01 2019
Journal Name
Journal Of Global Pharma Technology
Synthesis and Characterization of Some New Pyrazole Derivatives‏
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This work contain many steps starting from esterification of isophthalic acid to yield diester compound [I] which was converted to their acid hydrazide [II], then the later compound reacted with ethylacetoacetate to yield pyrazol-5-one compound [III]. Afterword added acetyl chloride to give the compound [IV], the reaction of this compound with theiosemicarbazide led to produce a new carbothioamide compound [V], which was reacted with ethyl chloro acetate to yield the thioxoimidazolidin compound [VI]. The condensation reactions of this compound with different substituted aldehyde give new alkene derivatives [VII] ad. The synthesized compounds were characterized by melting points, FT-IR, 1H-NMR and Mass spectroscopy.

Publication Date
Thu Aug 31 2023
Journal Name
Journal Of Wasit For Science And Medicine
Synthesis, Characterization and Antimicrobial Study of Polyacetal-Co complex/Nano Chitosan polymer blend
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Polycyclicacetal was prepared by the reaction of PEG with 4-nitrobenzaldehyde. Cobalt was used for producing a polymer metal complex and solution casting was used to produce a polymer blend including nano chitosan. All produced compounds have been characterized by FT-IR, DSC/ TGA, and SEM techniques as well as biological activity. The production of polyacetal is illustrated by the FT-IR analysis. The DSC/TGA results indicate the prepared polymer blends' thermal stability. Staphylococcus aureas, Klebsiella pneumoniae, Bacillus subtilis, and Escherichia coli were the four types of bacteria selected to study and evaluate the antibacterial activity of produced polyacetal, its metal complex, and polymer blend. Results indicates that ther

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Publication Date
Sat Nov 30 2024
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some Oxazolidine and Thiazolidine Derivatives and Study of their Antioxidants Activity
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 In this work, the preparation of some new oxazolidine and thiazolidine derivatives has been conducted. This was done over two steps; the first step included the synthesis of Schiff bases A1-A5 in 72-88% yields by the condensation of isonicotinic acid hydrazide and aldehydes. The second step includes the cyclization of derivatives A1-A5 with glycolic acid and thioglycolic acid to obtain the desired products, oxazolidine derivatives B1-B5 (44-60% yields) and thiazolidine derivatives C1-C5 (41-61% yields), respectively. The structure of the prepared compounds was characterized using FT-IR, 1H NMR, and 13C NMR spectroscopy. Some of the produced compounds were tested for antioxidant properties.  

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Publication Date
Fri Nov 01 2024
Journal Name
Current Medicinal Chemistry
Synthesis, In Silico Prediction, and In Vitro Evaluation of Anti-tumor Activities of Novel 4'-Hydroxybiphenyl-4-carboxylic Acid Derivatives as EGFR Allosteric Site Inhibitors
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Introduction:

Allosteric inhibition of EGFR tyrosine kinase (TK) is currently among the most attractive approaches for designing and developing anti-cancer drugs to avoid chemoresistance exhibited by clinically approved ATP-competitive inhibitors. The current work aimed to synthesize new biphenyl-containing derivatives that were predicted to act as EGFR TK allosteric site inhibitors based on molecular docking studies.

Methods:

A new series of 4'-hydroxybiphenyl-4-carboxylic acid derivatives, including hydrazine-1-carbothioamide (S3-S6) and 1,2,4-triazole (S7-S10) derivatives, were synthesized and characterized using IR, 1HNMR, 13CNMR

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Publication Date
Fri Jan 01 2016
Journal Name
Journal Of The College Of Basic Education
Simultaneous Determination of Cephalexin and Cefixime by First and Second Derivative Ultraviolet Spectrophotometry
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A new spectrophotometric method for individual and simultaneous determination of cefixime and cephalexin depending on the first and second derivative mode techniques. The first and second derivative spectra of these compounds permitted individual and simultaneous determination of cefixime and cephalexin in concentration interval of (4– 24μg.ml-1 ) by measuring the amplitude of peak-to-base line, pea to peak at certain wavelengths and the area under peak at selected spectrum intervals. The methods showed reasonable precision and accuracy and have been applied to determine cefixime and cephalexin in two different pharmaceutical preparations.

Publication Date
Sun Jan 03 2016
Journal Name
Journal Of The College Of Basic Education
Simultaneous determination of cephalexin and cefixime by first and second derivative ultraviolet spectrophotometry
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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
Tue Jan 01 2019
Journal Name
Biochem. Cell. Arch
BIOSYNTHESIS OF SILVER NANOPARTICLES USING MINTS LEAF EXTRACT AND EVALUATION OF THEIR ANTIMICROBIAL ACTIVITY
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The aim of this study is to synthesize an easy, non-toxic and eco-friendly method. Silver nanoparticles which were synthesized by leaf extract of mint were characterized by UV-Visible Spectroscopy which appears UVVisible spectrum of demonstrated a peak 448 nm corresponding to surface Plasmon resonance of silver nanoparticles, Fourier Transform Infrared Spectroscopy (FTIR); functional groups involved in the silver nanoparticles synthesis were identified, the presence of silver nanoparticles was confirmed by X-ray diffraction (XRD) and Atomic Force Microscope (AFM) analysis clearly illustrated that the shape of silver nanoparticles was spherical and the size of the silver nanoparticles has been measured as 55- 85 nm. Evaluation of its antimic

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Publication Date
Fri Dec 01 2023
Journal Name
Russian Journal Of Bioorganic Chemistry
A Brief Review on Schiff Base, Synthesis, and Their Antimicrobial Activities
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Publication Date
Sun Jan 01 2023
Journal Name
Materials Today: Proceedings
Preparation, characterization and preliminary cytotoxic evaluation of 6-mercaptopurine-coated biotinylated carbon dots nanoparticles as a drug delivery system
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