Journal ArticleDOI
One-pot synthesis and molecular docking of some new spiropyranindol-2-one derivatives as immunomodulatory agents and in vitro antimicrobial potential with DNA gyrase inhibitor
TLDR
The most potent compounds showed an increase in the intracellular killing activity of neutrophils which confirmed the immunostimulatory power, and compounds 7f showed the much better than norfloxacin with higher potency results.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2020-02-15. It has received 59 citations till now. The article focuses on the topics: DNA gyrase & Norfloxacin.read more
Citations
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Journal ArticleDOI
Oxindole and its derivatives: A review on recent progress in biological activities.
Yogesh Mahadu Khetmalis,Mithula Shivani,Sankaranarayanan Murugesan,Kondapalli Venkata Gowri Chandra Sekhar +3 more
TL;DR: In this paper, the authors provide a description of the general chemistry based on existing corresponding structureactivity relationships (SARs) and compile all recent developmentary studies on oxindole-derived compounds as a successful pharmaceutical agent.
Journal ArticleDOI
Antimicrobial evaluation of thiadiazino and thiazolo quinoxaline hybrids as potential DNA gyrase inhibitors; design, synthesis, characterization and morphological studies
Yousry A. Ammar,Awatef A. Farag,Abeer M. Ali,Sadia A. Hessein,Ahmed A. Askar,Eman A. Fayed,Doaa M. Elsisi,Ahmed Ragab +7 more
TL;DR: The most potent compounds 2, 7, 9, 10, 12 and 13c were exhibited bactericidal activity, in addition to fungistatic activity by dead live assay, and showed a significant result against all multi-drug resistance (MDRB) used especially compound 13c that displayed the best results with MICs of MDRB.
Journal ArticleDOI
Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity.
TL;DR: Immunomodulatory activities showed that the promising Schiff bases increase the immunomodulator effect of defense cell and the Schiff base 8a is the highest one by (Intra. killing activity = 136.5 ± 0.3%) having a pyrazole moiety as well as amide function (O=C-NH2) and piperidinyl core.
Journal ArticleDOI
Design, synthesis, in vitro antimicrobial evaluation and molecular docking studies of indol-2-one tagged with morpholinosulfonyl moiety as DNA gyrase inhibitors.
Mohamed A. Salem,Ahmed Ragab,Abeer El-Khalafawy,Abeer H. Makhlouf,Ahmed A. Askar,Yousry A. Ammar +5 more
TL;DR: A series of Schiff bases 3, 5, 7 and hydrazones 9 were achieved via reaction of 5-(morpholinosulfonyl)indol-2,3-dione with appropriate amines and/or hydrazide derivatives and enabled a better understanding of their structural features.
Journal ArticleDOI
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.
References
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Journal ArticleDOI
Javaniside, a novel DNA cleavage agent from Alangium javanicum having an unusual oxindole skeleton
Ji Ma,Sidney M. Hecht +1 more
TL;DR: Bioassay-guided fractionation of an extract prepared from Alangium javanicum using an assay to monitor Cu(2+)-dependent DNA strand scission led to the isolation of javaniside, a new type of oxindole glycoside.
Journal ArticleDOI
Synthesis and biological evaluation of some novel thiazole compounds as potential anti-inflammatory agents
Mohamed H. Helal,Mohamed A. Salem,Mohamed A. Salem,Mohamed S. A. El-Gaby,Mohamed S. A. El-Gaby,M. Aljahdali,M. Aljahdali +6 more
TL;DR: The structure of the newly compounds was confirmed on the basis of elemental analysis and spectral data and the inhibition of the carrageenin-induced oedema by these compounds was established.
Journal ArticleDOI
4-Quinolone derivatives and their activities against Gram positive pathogens
TL;DR: The enriched SAR paves the way to the further rational development of 4-quinolones with a unique mechanism of action different from that of the currently used drugs to overcome the resistance, well-tolerated and low toxic profiles.
Book ChapterDOI
The Theory of Antibiotic Inhibition Zones
TL;DR: This chapter presents the theory of antibiotic inhibition zones, and discusses the sequence of events that may occur when an antibiotic diffuses through agar in which bacterial cells capable of multiplying in the medium are present.
Journal ArticleDOI
Highly Efficient Enantioselective Construction of Bispirooxindoles Containing Three Stereocenters through an Organocatalytic Cascade Michael–Cyclization Reaction
TL;DR: Bispirooxindole derivatives containing three stereocenters, including two spiro quaternary centers, were synthesized in a high-yielding, atypically rapid, and stereocontrolled cascade Michael-cyclization reaction between methyleneindolinones and isothiocyanato oxindoles catalyzed by a bi- or multifunctional organocatalyst.