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bijps-386
Synthesis of New Cephalosporins of Expected Improved Activity and Resistance Against -Lactamases
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The development of new cephalosporins with improved activity against resistant microbes, such as, MRSA (methicillin resistant Staph. aureus), P. aeruginosa, is of high potential. Chemical synthesis of two new series of thiadiazole linked to cysteine (series 1) and cephalosporins containing thiadiazole linked to cysteine through disulfide bond (series 2) were achieved. The chemical structures of the synthesized compounds were confirmed using spectral (FT-IR, 1H-NMR) and elemental microanalysis. The incorporation of privileged chemical moieties, such as, thiadiazole, Schiff base, cysteine and sulfonamide, has been found to have great contribution to the antimicrobial activities. Compounds of series 1 (1b-d), containing a Schiff base or a sulfonamido moiety, showed reasonable activity and were less potent than cephalexin with respect to E. coli and Staph. aureus. The new cephalosporins (series 2) showed remarkable activities on E. coli (62.5-15.6µg/ml) and staph. aureus (31.2-62.5µg/ml) when compared with cephalexin (250 and 125 µg/ml) respectively. Moreover, compounds 1 and 3 showed very promising activity against MRSA (250 and 500µg/ml) respectively. The incorporation of a sulfonamido moiety to the cephalosporin molecule was successfully achieved. This is a very interesting finding which may open a new approach in the synthesis of newer cephalosporins.   

Keywords: Cephalosporins, Cysteine, Schiff base, Sulfonamides, Thiadiazole.

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Publication Date
Thu May 29 2025
Journal Name
Indonesian Journal Of Chemistry
Synthesis, Spectral Identification, Thermal Studies, Antioxidant Properties, and Biological Effects for Some Metal Ion Complexes with New Schiff Base Ligand
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The tetradentate N2O2 Schiff base ligand, which is produced via the condensation reaction of 2-hydroxynaphthaldehyde with phthalohydrazide, is prepared in this work with a fair yield. The prepared ligand was characterized using a microanalysis technique (C.H.N), UV-vis, FTIR, 1H-,13C-NMR, mass spectrometry, and thermal gravimetric analysis (TGA). New complexes were synthesized by a reaction between ligand (N'1E,N'2Z)-N'1,N'2-bis((1-hydroxynaphthalen-2yl)methylene)phthalohydrazide and metal chloride of Co+2, Ni+2, and Zn+2 ions in absolute ethanol. The present complexes are also characterized by techniques such as C.H.N, UV-vis, FTIR, TGA, molar conductivity, atomic absorption, and magnetic moment measurements. The in vitro antimicro

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Publication Date
Thu Dec 15 2022
Journal Name
Bionatura
Antibiogram of Eucalyptus and Sesame seed oil against clinical isolates of Pseudomonas aeruginosa
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Publication Date
Mon Apr 10 2023
Journal Name
The European Physical Journal Plus
Improved performance of D149 dye-sensitized ZnO-based solar cell under solvents activation effect
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Publication Date
Sun Feb 25 2024
Journal Name
Baghdad Science Journal
An Improved Cuckoo Search Algorithm for Maximizing the Coverage Range of Wireless Sensor Networks
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The issue of increasing the range covered by a wireless sensor network with restricted sensors is addressed utilizing improved CS employing the PSO algorithm and opposition-based learning (ICS-PSO-OBL). At first, the iteration is carried out by updating the old solution dimension by dimension to achieve independent updating across the dimensions in the high-dimensional optimization problem. The PSO operator is then incorporated to lessen the preference random walk stage's imbalance between exploration and exploitation ability. Exceptional individuals are selected from the population using OBL to boost the chance of finding the optimal solution based on the fitness value. The ICS-PSO-OBL is used to maximize coverage in WSN by converting r

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Publication Date
Wed Jun 30 2021
Journal Name
International Journal Of Intelligent Engineering And Systems
Promising Gains of 5G Networks with Enhancing Energy Efficiency Using Improved Linear Precoding Schemes
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Publication Date
Sun Oct 01 2017
Journal Name
Ieee Transactions On Neural Systems And Rehabilitation Engineering
A Framework of Temporal-Spatial Descriptors-Based Feature Extraction for Improved Myoelectric Pattern Recognition
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Publication Date
Thu Sep 26 2013
Journal Name
Chemistry: The Key To Our Sustainable Future
Synthesis and Characterization of Some New Metal Complexes of Condensation Reaction Products of 3-Amino-1,2,4-Triazole with Isatin, N-Acetylisatin and Bis (2,3-Dioxoindolin-1-yl)Mercury(II)
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Publication Date
Fri Dec 20 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Sulfur Derivatives of 1,2,4-Triazole: Recently Developed Compounds, Structure Activity Relationship, and Biological Activity: Review article
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The term of heterocyclic chemistry focuses only on heterocyclic compounds, which consider as a percentage of organic chemistry, they equal to greater than sixty-five. These compounds are widely founded in nature and most of them are important to life. In the past few years, scientist fused on 1,2,4-triazoles and their condensed heterocyclic ring due to their medicinal significance, 1,2,4-triazole containing Sulphur atom is one of the important heterocyclic moieties due to its broad range of biological activities also their derivatives can accommodate one of the alternatives as electronic effect as exchanges of the electronic density (electron donating or withdrawing) groups ; for all what mentioned above they are consider as a core

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences
Synthesis of new conjugates of some NSAIDs with sulfonamide as possible mutual prodrugs using tyrosine spacer for colon targeted drug delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)

Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis of new Conjugates of some NSAIDs with Sulfonamide as Possible Mutual Prodrugs using Tyrosine Spacer for Colon Targeted Drug Delivery
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The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of  inflammation and infections in colon).

Key words: Mutual prodrug, Ester linkage, Azo bond, Colon targeting

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