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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
Sat Aug 15 2015
Journal Name
Chemistry And Materials Research
Synthesis and Characterization of 3, 5-Dimethyl-2-(4-nitrophenyl azo)-Phenol Complexes with Co (II) and Ni (II) and Study Its Effect on the Activity of Ach Enzyme (invitro)
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Publication Date
Mon Jan 01 2024
Journal Name
Polski Merkuriusz Lekarski
Design, synthesis, insilco study and biological evaluation of new isatin-sulfonamide derivatives by using mono amide linker as possible as histone deacetylase inhibitors
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Aim: To evaluate the cytotoxic activity of newly synthesized a series of novel HDAC inhibitors comprising sulfonamide as zinc binding group and Isatin derivatives as cap group joined by mono amide linker as required to act as HDAC inhibitors. Materials and Methods: The utilization of sulfonamide as zinc binding group joined by N-alkylation reaction with ethyl-bromo hexanoate as linker group that joined by amide reaction with Isatin derivatives as cap groups which known to possess antitumor activity in the designed of new histone deacetylase inhibitors and using the docking and MTT assay to evaluate the compounds. Results: Four compounds have been synthesized and characterized successfully by ART-FTIR, NMR and ESI-Ms. the compounds w

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Publication Date
Sun May 10 2020
Journal Name
Baghdad Science Journal
Molecular Analysis of Rifampicin Resistance Conferring Mutations in Mycobacterium tuberculosis
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Mycobacterium tuberculosis resistance to rifampicin is mainly mediated through mutations in the rpoB gene. The effects of rpoB mutations are relieved by secondary mutations in rpoA or rpoC genes. This study aims to identify mutations in rpoB, rpoA, and rpoC genes of Mycobacterium tuberculosis isolates and clarify their contribution to rifampicin resistance. Seventy isolates were identified by acid-fast bacilli smear, Genexpert assay, and growth on Lowenstein Jensen medium. Drug susceptibility, testing was performed by the proportional method.  DNA extraction, PCR, and sequencing were accomplished for the entire rpoA, rpoB, and

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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
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 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
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
Fri Dec 01 2023
Journal Name
Slas Discovery
Role Of Vaccines Against COVID-19 Pandemic
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Publication Date
Fri Aug 10 2018
Journal Name
Ceramics International
Application of zirconia surface coating to improve fracture resistance and stress distribution of zirconia ceramic restorations
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Zirconia ceramic restoration (ZCR) has a higher fracture incidence rate than metal ceramic restoration. Different surface treatments were used to improve fracture performance of ZCR such as grit blasting (GB) by aluminium oxide powder. This type of surface treatment generate residual stresses on veneering ceramic causing crack initiation and ending with a fracture. In order to overcome the stress generated by GB, zirconia surface coating is used as a surface treatment to improve fracture resistance and to accommodate stresses along the ZCR layers. Fifty zirconia ceramic crowns were fabricated and divided according to the type of surface treatment into three groups; the first group is (ZG), involving 20 cores were coated with a mixture of pa

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Publication Date
Mon Jan 01 2024
Journal Name
Baghdad Science Journal
Preparation and Characterization of Silver Nanoparticles and its Medical Application against Pathogenic Bacteria
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The fabrication of Solid and Hollow silver nanoparticles (Ag NPs) has been achieved and their characterization was performed using transmission electron microscopy (TEM), zeta potential, UV–VIS spectroscopy, and X-ray diffraction (XRD). A TEM image revealed a quasispherical form for both Solid and Hollow Ag NPs. The measurement of surface charge revealed that although Hollow Ag NPs have a zeta potential of -43 mV, Solid Ag NPs have a zeta potential of -33 mV. According to UV-VIS spectroscopy measurement Solid and Hollow Ag NPs both showed absorption peaks at wavelengths of 436 nm and 412 nm, respectively. XRD pattern demonstrates that the samples' crystal structure is cubic, similar to that of the bulk materials, with

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