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Synthesis of new derivatives of Ceftazidime as possible Prodrugs
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Five new ceftazidime derivatives were designed and synthesized in an attempt to improve the acid stability and may increase the spectrum of ceftazidime. The synthesized compounds included;  Schiff base of ceftazidime (compound 1), ceftazidime lysine amide Schiff base (compound 2), ceftazidime lysine amide (compound 3), ceftazidime-di-lysine amide Schiff base (compound 4) and ceftazidime-di-lysine amide (compound 5). New ceftazidime derivatives were successfully prepared characterized and identified using spectral and elemental microanalysis (CHNS) analyses and the results comply with the calculated measurements.

Compounds 1 and 2 were subjected to a stability study in phosphate buffer (0.2M, pH 7.4) and in KCl/HCl buffer (0.2M, pH 1.2) at different time intervals (0 – 240 min) incubated at 37 °C. This revealed that both compounds in phosphate buffer (0.2M, pH 7.4) are significantly stable with t 1/2 of 18hrs and 24hrs respectively. However, compounds 1 and 2 are less stable in KCl/HCl buffer (0.2M, pH 1.2) with t1/2 of 3.48hrs and 3.13hrs respectively.

The antibacterial evaluation of the new ceftazidime derivatives showed various degrees of antibacterial activities when compared with ceftazidime. The chemical modifications of ceftazidime showed slight effect on activities and most of compounds retained the antibacterial activities. Compounds 2 and 4  afforded comparable antibacterial action. However, compounds 3 and 5 were equipotent with ceftazidime with respect to E.coli and Staph. aureose. Compound 4 has better activity than ceftazidime with respect to Pseudomonas  aeruginosa. Schiff's base derivative of lysine (2, 6-bis-(benzylideneamino) hexanoic acid) gave a reasonable antibacterial action towards Escherichia coli and Streptococcus Spp; as compared with lysine which has no antibacterial activity.

Key words: Ceftazidime, Schiff bases, Lysine.

 

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Publication Date
Sun Oct 20 2024
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Investigation The Biological Activity of Some New Alkenes Based on Thiazoldin-4-one Compounds
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This work has been done to prepare a series of new alkene compounds derived from 4-thiozolidinones by substituting different aldehydes, P-acetamido-phenol, and 2-mercapto-benzoimidazole, which were used as starting materials to form ester [I]a,b and then make hydrazides [II]a,b, which were used to prepare 1, 3, and 4-oxadiazoles [III]a,b, which were then used for prepared Schiff bases [IV]a-f, The next step was the synthesis of 4-thiazoldinone derivatives [V]a-f  from Schiff bases. The final step was the synthesis of alkenes [VII]a-f, the prepared derivatives were identified with spectral methods (FT-IR, 1H-NMR, mass, and CHNS). The antibacterial activity of the prepared derivatives was evaluated against four types of bacteria, pos

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Publication Date
Thu Oct 31 2019
Journal Name
Asian Journal Of Pharmaceutical And Clinical Research
DESIGN, SYNTHESIS, DOCKING, ANTITUMOR SCREENING, AND ABSORPTION, DISTRIBUTION, METABOLISM, AND EXCRETION PREDICTION OF NEW HESPERDIN DERIVATIVE
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Objective: Hesperidin (HSP) is a pharmacologically active organic compound found in citrus fruits and peppermint. We synthesized a new HSP derivative by reacting it with 5-Amino-1,3,4-thiadiazole-2-thiol in acetic acid. Methods: This compound was characterized by Fourier-transform infrared, proton nuclear magnetic resonance, and electron impact mass spectra. A molecular docking study explores the predicted binding of the compound and its possible mode of action. Bioavailability, site of absorption, drug mimic, and topological polar surface was predicted using absorption, distribution, metabolism, and excretion (ADME) studies. Results: The docking study predicts that the new compound binds to the active sites of Aurora-B

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Publication Date
Tue Oct 26 2021
Journal Name
Egyptian Journal Of Chemistry
Synthesis of new polymers linked to heterocyclic using zinc oxide with nanostructures extracted from natural sources
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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
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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

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Publication Date
Sun Jul 01 2001
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
New record of ground pearls, Porphyrophora tritici (Bod.) (Homoptera, Margarodidae) as a pest of wheat in Iraq
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The ground pearls, Porphyrophora tritici (Bod.) is a new insect pest on wheat recorded for
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Publication Date
Tue May 19 2026
Journal Name
Al-mustansiriyah Journal Of Science
Epidemiological Study to Investigate a Possible Vector of Visceral Leishmaniasisin the Central Region of Iraq
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An epidemiological study in Al-Mahmmodiya (50 km south Baghdad) to investigate a possible vector of Leishmaniasis were applied .This region is considered as a foci of Leishmaniasisaccording to the health association statistics. CDC light traps were used to collect the insects nightly. Insects were collected by Indoor application as human dwellings and animal shelters and Outdoor application as rodent's barrows and field trees. Sand flies were transported to the laboratory, isolated and identified according to the identification keys in Tropical Biological Researches Unit at the Collage of Science / University of Baghdad. Must of the collected sand flies were belonging to three species PhlebotomuspapatasiScopoli(45%), PhlebotomusalexandriSin

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Publication Date
Sat Aug 01 2015
Journal Name
Journal Of Sol-gel Science And Technology
Synthesis and spectroscopic properties of silica nanoparticles as scatter centers in random gain porous media
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Publication Date
Fri Jan 01 2021
Journal Name
Materials Today: Proceedings
Synthesis of gamma biguanides butyric acid analogues as HDAC inhibitors and studying their cytotoxic activity
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Publication Date
Tue Sep 01 2020
Journal Name
Optik
Synthesis of Ag2O films by pulsed laser deposited on porous silicon as gas sensor application
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Publication Date
Tue Jul 01 2025
Journal Name
International Journal Of Corrosion And Scale Inhibition
Synthesis of bis chromene derivative as a dual-functional corrosion inhibitor and CDK2 targeting agent
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