Journal ArticleDOI
Hydrazonoyl bromide precursors as DHFR inhibitors for the synthesis of bis-thiazolyl pyrazole derivatives; antimicrobial activities, antibiofilm, and drug combination studies against MRSA.
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TLDR
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.About:
This article is published in Bioorganic Chemistry.The article was published on 2021-09-13. It has received 34 citations till now. The article focuses on the topics: Antimicrobial & Pyrazole.read more
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Development of novel indolin-2-one derivative incorporating thiazole moiety as DHFR and quorum sensing inhibitors: Synthesis, antimicrobial, and antibiofilm activities with molecular modelling study
TL;DR: In this paper , a series of new thiazolo-indolin-2-one derivatives were synthesized based on acid and base catalyzed condensation or reaction of thiosemicarbazone 8 with different electrophilic reagents.
Journal ArticleDOI
One-Pot Synthesis and Molecular Modeling Studies of New Bioactive Spiro-Oxindoles Based on Uracil Derivatives as SARS-CoV-2 Inhibitors Targeting RNA Polymerase and Spike Glycoprotein
Samar A. El-Kalyoubi,Ahmed Ragab,Ola A. Abu Ali,Yousry A. Ammar,Mohamed G. Seadawy,Aya Ahmed,Eman A. Fayed +6 more
TL;DR: This study aims to design a simple and efficient cyclo-condensation reaction of 6-aminouracil derivatives 2a–e and isatin derivatives 1a–c to synthesize spiro-oxindoles 3a–d, 4 a–e, and 5a-e to synthesise spiro’s most active hybrids.
Journal ArticleDOI
Design, synthesis of new novel quinoxalin-2(1H)-one derivatives incorporating hydrazone, hydrazine, and pyrazole moieties as antimicrobial potential with in-silico ADME and molecular docking simulation
Ahmed Ragab,Doaa M. Elsisi,Ola A. Abu Ali,Moustafa S. Abusaif,Ahmed A. Askar,Awatef A. Farag,Yousry A. Ammar +6 more
TL;DR: A series of 6-(morpholinosulfonyl)quinoxalin-2(1H)-one based hydrazone, hydrazine, and pyrazole moieties were designed, synthesized, and evaluated for their in vitro antimicrobial activity.
Journal ArticleDOI
Design, synthesis, molecular modeling, and antimicrobial potential of novel 3-[(1H-pyrazol-3-yl)imino]indolin-2-one derivatives as DNA gyrase inhibitors.
Abdullah Y. Alzahrani,Yousry A. Ammar,Mohamed A. Salem,Mohamed A. Salem,Mohammed Abu-Elghait,Ahmed Ragab +5 more
TL;DR: A series of 3]-(1H-pyrazol-3-yl)imino]-indolin-2-one derivatives were designed using the molecular hybridization method, characterized using different spectroscopic techniques, and evaluated for their in vitro antimicrobial activity.
Journal ArticleDOI
Design, synthesis of new novel quinoxalin-2(1H)-one derivatives incorporating hydrazone, hydrazine, and pyrazole moieties as antimicrobial potential with in-silico ADME and molecular docking simulation
TL;DR: A series of 6-(morpholinosulfonyl)quinoxalin-2(1 H )-one based hydrazone, hydrazine, and pyrazole moieties were designed, synthesized, and evaluated for their in vitro antimicrobial activity as mentioned in this paper .
References
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Journal ArticleDOI
Will 10 Million People Die a Year due to Antimicrobial Resistance by 2050
TL;DR: Marlieke de Kraker and colleagues reflect on the need for better global estimates for the burden of antimicrobial resistance and suggest that more needs to be done to estimate this burden.
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Correction: Corrigendum: Novel anti-thrombotic agent for modulation of protein disulfide isomerase family member ERp57 for prophylactic therapy
Guozhen Cui,Luchen Shan,Lin Guo,Ivan K. Chu,Guohui Li,Quan Quan,Yun Zhao,Cheong Meng Chong,Zaijun Zhang,Pei Yu,Maggie Pui Man Hoi,Yewei Sun,Yuqiang Wang,Simon Ming-Yuen Lee +13 more
TL;DR: ADTM represents a promising candidate for anti-thrombotic therapy targeting ERp57, a novel derivative of danshensu that displayed strong cardioprotective effects against oxidative stress-induced cellular injury in vitro and acute myocardial infarct in vivo.
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Effect of different drying techniques on flowability characteristics and chemical properties of natural carbohydrate-protein Gum from durian fruit seed.
TL;DR: The present study revealed that freeze drying among all drying techniques provided the most desirable functional properties and flow characteristics for durian seed gum.
Journal ArticleDOI
Dihydrofolate reductase as a therapeutic target.
TL;DR: Progress has been made recently in understanding the biochemical basis for the selectivity of this drug and the biochemical mechanism (or mechanisms) responsible for the development of resistance to treatment with the drug, which has led to a new generation of DHFR inhibitors that are now in clinical trials.