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
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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.
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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.
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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.
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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.
References
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The Asymmetric Total Synthesis of (+)- and (−)-Spirotryprostatin B
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Neutrophils and Host Defense
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A new structural alternative in benzo[b]furans for antimicrobial activity.
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