Sulfaguanidine Hybrid with Some New Pyridine-2-One Derivatives: Design, Synthesis, and Antimicrobial Activity against Multidrug-Resistant Bacteria as Dual DNA Gyrase and DHFR Inhibitors.
Ahmed Ragab,Sawsan A. Fouad,Ola A. Abu Ali,Entsar M. Ahmed,Abeer M. Ali,Ahmed A. Askar,Yousry A. Ammar +6 more
TLDR
In this article, a series of hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a-d, pyridine-2-one 3-10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis.Abstract:
Herein, a series of novel hybrid sulfaguanidine moieties, bearing 2-cyanoacrylamide 2a-d, pyridine-2-one 3-10, and 2-imino-2H-chromene-3-carboxamide 11, 12 derivatives, were synthesized, and their structure confirmed by spectral data and elemental analysis All the synthesized compounds showed moderate to good antimicrobial activity against eight pathogens The most promising six derivatives, 2a, 2b, 2d, 3a, 8, and 11, revealed to be best in inhibiting bacterial and fungal growth, thus showing bactericidal and fungicidal activity These derivatives exhibited moderate to potent inhibition against DNA gyrase and DHFR enzymes, with three derivatives 2d, 3a, and 2a demonstrating inhibition of DNA gyrase, with IC50 values of 1817-2387 µM, and of DHFR, with IC50 values of 433-554 µM; their potency is near to that of the positive controls Further, the six derivatives exhibited immunomodulatory potential and three derivatives, 2d, 8, and 11, were selected for further study and displayed an increase in spleen and thymus weight and enhanced the activation of CD4+ and CD8+ T lymphocytes Finally, molecular docking and some AMED studies were performedread more
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Design, synthesis, antiproliferative evaluation, and molecular docking study of new quinoxaline derivatives as apoptotic inducers and EGFR inhibitors
Eman A. Fayed,Yousry A. Ammar,Marwa A. Saleh,Ashraf H. Bayoumi,Amany Belal,Amany Belal,Ahmed B.M. Mehany,Ahmed Ragab +7 more
TL;DR: A new series of quinoxaline derivatives synthesized and pharmacologically evaluated against (HepG-2, HCT-116, and MCF-7) cell lines and revealed that it increases apoptotic cells and induced cell cycle arrest at pre-G1 and G2/M phases.
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Hydrazonoyl bromide precursors as DHFR inhibitors for the synthesis of bis-thiazolyl pyrazole derivatives; antimicrobial activities, antibiofilm, and drug combination studies against MRSA.
TL;DR: In this article, a series of new bis-thiazolyl-pyrazole derivatives 3, 4a-c, 5a, b, and 6a -c was synthesized by reacting bis hydrazonoyl bromide with several active methylene reagents in a one-pot reaction.
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Design, synthesis of new magenta dyestuffs based on thiazole azomethine disperse reactive dyes with antibacterial potential on both dyes and gamma-irradiated dyed fabric
TL;DR: In this paper, a series of new magenta azomethine reactive disperse dyes were synthesized and applied into polyester/cotton blend fabrics, and various spectroscopic and analytical techniques characterized all the synthesized dyes.
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Development of adamantane scaffold containing 1,3,4-thiadiazole derivatives: Design, synthesis, anti-proliferative activity and molecular docking study targeting EGFR.
Mohammed M.S. Wassel,Yousry A. Ammar,Gameel A. M. El-Hag Ali,Amany Belal,Ahmed B.M. Mehany,Ahmed Ragab +5 more
TL;DR: Thiazolo-thiadiazole adamantane derivative 17 exhibited the strongest inhibitory activity to the EGFR, which proved their role as hopeful apoptotic inducers in this research work.
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One-pot strategy for thiazole tethered 7-ethoxy quinoline hybrids: Synthesis and potential antimicrobial agents as dihydrofolate reductase (DHFR) inhibitors with molecular docking study
Yousry A. Ammar,Sondos M.A. Abd El-Hafez,Sadia A. Hessein,Abeer M. Ali,Ahmed A. Askar,Ahmed Ragab +5 more
TL;DR: Molecular docking study against DHFR enzyme (1DLS) was carried out, and the active derivatives bind to some the nearly the same amino acid residues as MTX that support the hypothesis that quinoline antibiotic class can be solved by discovering new targets and inhibitors.
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The Immune System
TL;DR: If a mouse is injected subcutaneously with a suspension of appropriate bacteria, either the mouse falls ill and succumbs to the infection within a few days, or it recovers and is found to be resistant to any subsequent attempts at reinfection with the same type of bacterium.