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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
Fri Aug 18 2023
Journal Name
Medicinal Chemistry Research
New tolfenamic acid derivatives with hydrazine-1-carbothioamide and 1,3,4-oxadiazole moieties targeting VEGFR: synthesis, in silico studies, and in vitro anticancer assessment
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Publication Date
Thu Jun 01 2023
Journal Name
Measurement: Sensors
Improved airborne computer system strategy for swarm drones flying based on skybrush suite and inspired technique
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Publication Date
Sun Sep 25 2022
Journal Name
Research Journal Of Chemistry And Environment
Synthesis, Antioxidant ability and Docking study for new 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))diphenol)
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New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydr

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Publication Date
Mon Oct 10 2022
Journal Name
Research Journal Of Chemistry And Environment
Synthesis, Antioxidant ability and Docking study for new 4,4'-((2-(Aryl)-1H-benzo[d]imidazole-1,3(2H)- diyl)bis(methylene))diphenol)
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New series of 4,4'-((2-(Aryl)-1H-benzo[d]imidazole1,3(2H)-diyl)bis(methylene))Diphenol(3a-g) was successfully synthesized from cyclization of the reduction product of bis Schiff bases (2) with aryl aldehydes bearing phenolic hydroxyl in the presence of acetic acid. The structure of these compounds was identified from FT-IR, 1H NMR, 13C NMR and EIMs. The Antioxidant capability was screened by DPPH and FRAP assays. Both assays showed antioxidant capability more than BHT as well. Compounds 3b and 3c showed antioxidant capacity slightly less than ascorbic acid. The docking study for theses compound was carried out as III DNA polymerase inhibitor. The results of docking demonstrated that the increase in hinderances around phenolic hydroxyl for t

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Publication Date
Sun Dec 01 2024
Journal Name
Russian Journal Of General Chemistry
Synthesis, Characterization, and Biological Evaluation for New Derivatives Based on 2Сhloro-N-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl]acetamide
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Publication Date
Sun Dec 01 2024
Journal Name
Russian Journal Of General Chemistry
Synthesis, Characterization, and Biological Evaluation for New Derivatives Based on 2Сhloro-N-[4-(5-phenyl-1,3,4-oxadiazol-2-yl)phenyl]acetamide
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Publication Date
Sun May 10 2020
Journal Name
Baghdad Science Journal
Investigation of the Biochemical and Ultrastructural Mechanisms Underlying the Antimicrobial Activity of Mimusops spp. Extracts: Antimicrobial activity of Mimusops spp.
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Antibiotic resistance is the major growing threat facing the pharmacological treatment of bacterial infections. Therefore, bioprospecting the medicinal plants could provide potential sources for antimicrobial agents. Mimusops, the biggest and widely distributed plant genus of family Sapotaceae, is used in traditional medicines due to its promising pharmacological activities. This study was conducted to elucidate the antimicrobial effect of three unexplored Mimusops spp. (M. kummel, M. laurifolia and M. zeyheri). Furthermore, the mechanisms underlying such antibacterial activity were studied. The Mimusops leaf extracts revealed significant antibacterial activities against the five tested bacter

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Publication Date
Thu Aug 15 2019
Journal Name
Scholarspace
Folklore as Resistance in Postcolonial Narratives and Cultural Practices: Hawaiian, African American, and Iraqi
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Colonialism radically transformed the cultures of colonized peoples, often rupturing Indigenous traditions and folklore. Whether creating colonial discourse, promoting orientalist literature, advocating western educational institutions, or through biased media representations, imperial powers systematically oppressed Indigenous and Native peoples. Subjugated communities, however, created, and still form postcolonial discourse from their knowledge systems. This discourse insists on Indigenous and Native culture as central to Indigenous and Native peoples identity. This study examines the postcolonial literature of three groups: Kānaka Maoli, African Americans, and Iraqis. The scope of this dissertation scrutinizes how folklore is employed

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Publication Date
Thu Jan 07 2021
Journal Name
Jordan Journal Of Biological Sciences
Evaluation of Quorum-Sensing, Antibiotics Resistance, and Biofilm Formation in Pathogenic Bacteria from the Hospital Environments
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Abstract Background: Multidrug-resistant bacteria (MDR) often contaminate hospital environment and cause serious illnesses. Quorum Sensing (QS) regulates a variety of downstream cellular processes, including antibiotics resistance mechanisms and biofilm formation, and causes harm to the host. This study investigates antibacterial susceptibility and biofilm formation of pathogenic bacteria in hospital environment. Methods: Hundred bacterial isolates were collected from various environments in the Medical City hospital. The antimicrobial susceptibility technique was evaluated through disk diffusion method. Next, biofilms formation was detected by the microliter plate assay. Finally, PCR was used to analyze the frequency of QS system gene

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Publication Date
Thu Jun 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Marginal Discrepancy and Fracture Resistance of CAD/CAM Ceramill Sintron Metal Copings with Different Porcelain Materials
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Background: This study was performed to compare the marginal fit changes and facture resistance of metal ceramic crowns constructed from Ceramill Sintron metal coping veneered with three different porcelain veneering materials (Vita Master Koromikos VMK, Willi Geller Creation CC and GC initial MC), also to evaluate the influence of thermocycling on load at fracture. Materials and Methods: Master brass die was scanned ,then metal coping was designed and milled from Ceramill Sintron blank to get 60 metal copings, then divided randomly into three groups(20 sample), then veneered with porcelain: VITA, Creation or GC. The marginal gaps were measured before and after porcelain veneering then marginal fit changes was calculated. Fracture resist

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