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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 Jun 05 2016
Journal Name
Baghdad Science Journal
Synthesis of New Some Imidazole Derivatives Containing ?-Lactam Ring
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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.

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Publication Date
Fri Mar 01 2024
Journal Name
Baghdad Science Journal
Synthesis and Characterization of New 2-amino-5-chlorobenzothiazole Derivatives Containing Different Types of Heterocyclic as Antifungal Activity
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Nine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5  then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative

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Publication Date
Thu Jun 01 2023
Journal Name
Medicinal Chemistry
New Niflumic Acid Derivatives as EGFR Inhibitors: Design, Synthesis, In silico Studies, and Anti-proliferative Assessment
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Background:

1,3,4-oxadizole and pyrazole derivatives are very important scaffolds for medicinal chemistry. A literature survey revealed that they possess a wide spectrum of biological activities including anti-inflammatory and antitumor effects.

Objectives:

To describe the synthesis and evaluation of two classes of new niflumic acid (NF) derivatives, the 1,3,4-oxadizole derivatives (compounds 3 and (4A-E) and pyrazole derivatives (compounds 5 and 6), as EGFR tyrosine kinase inhibitors in silico and in vitro.

Methods:

The designed compounds were synthesized using convent

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Publication Date
Sun Mar 12 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of Some New Hydrazides and Their Derivatives
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New hydrazide compounds (A2) and (A9) were prepared from their corresponding esters (A1, A8) .These esters were also prepared from their precursors 5-ethoxy carbonyl-(4methoxyphenyl)-6-methyl-1,2,3,4-tetrahydropyrimidine-2-thione (A1) via multicomponent reaction type and from hippuric acid respectively. The hydrazide compounds were then allowed to react with some aldehydes forming the corresponding hydrazones (A3-7) and (A1014). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectroscopies and well discussed. .

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Publication Date
Sun Apr 23 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and antimicrobial evaluation of new 1,3,4 – Thiadiazole Derivatives
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The amino thiadiazole [I] on treatment with aromatic aldehydes yielded Schiff bases [IIa-c] , which cyclized to thiazolidinone [IIIa-c] derivatives by reaction with thioglycolic acid .Reaction of carbon disulfide and methyl iodide with [I] gavedithiomethyl[IV] which on treatment with o-phenylenediamine gave the condensed N-Imidazolythiadiazolylamine [V] , However , reaction of [I] with phenylisocyanate and phenylisothiocyanate afforded the carbamideand carbothiamide derivatives[VI.VII]a-c. The structure of these compounds was characterized from their  melting point , FTIR spectroscopy and elementalanalysis

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Publication Date
Fri Nov 24 2023
Journal Name
Iraqi Journal Of Science
Synthesis and characterization of some New Derivatives from 2- Mercaptobenzothiazole
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In this work 2- mercaptobenzothiazole ( 2-MBT ) and some of its derivatives(1, 14 ,27) were prepared by using home made Auto clave .The synthesis involve treatment of 2- MBT or some of its derivatives with chloro acetyl chloride to give 1- chloro acetyl -2- MBT or the corresponding derivatives (2,15,28) . the product was treated with phenyl hydrazine to give the phenyl hydrazide derivatives (3,16,29) . The new derivatives(4-13, 17-26,30-39) were synthesized by reaction of the phenyl hydrazide derivatives with different aromatic aldehydes in the presence of Acetic Acid . Structure of all the prepared compounds confirmation were proved using FTIR , elemental analysis (C .H .N .S ) in addition to melting points.

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Publication Date
Mon Aug 07 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Preliminary Pharmacological Evaluation of Some New Triazole Derivatives
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  On the basis of the results which was previously obtained from the structural and the theoretical studies on ~-adrenergic drugs, a series of 2-propanolamine derivatives containing triazole moiety have been prepared and evaluated for their cardiovascular activity . These derivatives were tested by using spontaneously-beating right atria of albino rats.

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Publication Date
Tue Dec 29 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization, and Antibacterial Evaluation of New Vanillic Acid Derivatives
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Publication Date
Mon Jun 03 2019
Journal Name
Journal Of Global Pharma Technology
New Diquinazoline Derivatives: Synthesis and Evaluation of AntiBacterial Activi
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Oxazine and quinazoline has a very important in organic chemistry especially in hetero cyclic fields. this research consist the preparation of 4H,4'H-2,2'-bibenzo[d][1,3]oxazine-4,4'-dione compound (1) from di acid chloride with 2-aminobenzoic acid in pyridine as solvent to give compound (2) 3,3'-diamino-2,2'- biquinazoline-4,4'(3H,3'H)-dione .compound 2 include free amino group .this compound was reacted with maleic and phthalic anhydride for synthesized of cyclic imide compounds (3,4).another reaction for compound 2 with some substituted aromatic aldehyde for prepared of some novel Schiff bases (5-9) contains quinazoline ring. compound 1 was treated with sulfathiazole and sulfadiazine for synthesized of sulfa compounds contains sulf

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Publication Date
Sat Jun 03 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Derivatives From 2-Mercaptobenzoxazole
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In this work 2-mercaptobenzoxazole (2-MBO) (1), was prepared by using homemade Auto clave .The synthesis involve treatment of 2-MBO with 2-chloro acetyl chloride to give 2-chloroacetyl thio benzoxazole (2), the product was treated with phenyl hydrazine to give 2-phenyl hydrazide acetyl thio benzoxazole (3). The new derivatives (4-13) were synthesized by reaction of 2-phenyl hydrazide acetyl thio benzoxazole (3) with different aromatic aldehydes in the presence of acetic acid. The compound (2) was treated with hydrazine hydrate to give product (14) then treated with different aromatic aldehydes in the presence of glacial acetic acid to give Schiff bases derivatives (15-24). Structure of all the prepared compounds confirmation were proved

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