Journal ArticleDOI
New Coumarin-Pyrazole hybrids: Synthesis, Docking studies and Biological evaluation as potential cholinesterase inhibitors
Amina Benazzouz-Touami,xiang zheng,Amina Chouh,Sabrina Halit,Souhila Terrachet-Bouaziz,Malika Makhloufi-Chebli,Karima Ighil-Ahriz,Artur M. S. Silva +7 more
TLDR
In vitro studies showed that compounds 3e and 3f were the most effective showing high potential AChE inhibitory activities with respective IC50 values, and in silico predictions of toxicity analysis indicated that these compounds should have good oral bioavailability.About:
This article is published in Journal of Molecular Structure.The article was published on 2022-02-05. It has received 13 citations till now. The article focuses on the topics: Chemistry & Butyrylcholinesterase.read more
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Design, synthesis, in vitro anticancer and antimicrobial evaluation, SAR analysis, molecular docking and dynamic simulation of new pyrazoles, triazoles and pyridazines based isoxazole
Hyam A. Radwan,Iqrar Ahmad,Ismail M.M. Othman,Mohamed A. M. Gad-Elkareem,Harun M. Patel,Kais Aouadi,Mejdi Snoussi,Adel Kadri +7 more
TL;DR: In this article , a series of pyrazoles, triazoles and pyridazines based isoxazole were synthesized, and well characterized, and the properties of these compounds were evaluated.
Journal ArticleDOI
“Pyrazolo-Imidazolidinones: Synthesis, Antimicrobial Assessment and Molecular Modelling Studies by Molecular Mechanic and Quantum Mechanic Approach”
Nisheeth C. Desai,Surbhi B. Joshi,Ashvinkumar G. Khasiya,Dharmpalsinh J. Jadeja,H K Mehta,Medha Pandya,Iqrar Ahmad,Harun M. Patel +7 more
TL;DR: In this paper , a set of fifteen pyrazole-imidazolidinone hybrids were synthesized and tested for antimicrobial activity, and the results showed that the compounds 4f with MIC (Minimum Inhibitory Concentration) 12.5 μg/mL against A. clavatus and 4l with MIC 12.6 μg /mL against P. aeruginosa were the most active compared to the standard drugs.
Journal ArticleDOI
Diverse and efficient catalytic applications of new cockscomb flower-like Fe3O4@SiO2@KCC-1@MPTMS@CuII mesoporous nanocomposite in the environmentally benign reduction and reductive acetylation of nitroarenes and one-pot synthesis of some coumarin compounds
TL;DR: In this paper , a new cockscomb flower-like mesoporous nanocomposite was prepared and characterized by various techniques including Fourier transform infrared (FT-IR) spectroscopy, powder X-ray diffraction (PXRD), scanning electron microscopy (SEM), SEM-based energy-dispersive X -ray (EDX) spectrography, inductively coupled plasma-optical emission spectrometry (ICP-OES), thermogravimetric analysis/differential thermal analysis (TGA/DTA), vibrating sample magnetometry (VSM), UV-Vis spectroscope, and Brunauer-Emmett-Teller (BET) and Barrett-Joyner-Halenda (BJH) analyses.
Journal ArticleDOI
Development of spiro-3-indolin-2-one containing compounds of antiproliferative and anti-SARS-CoV-2 properties
Nehmedo G. Fawazy,Siva S. Panda,Ahmed Mostafa,Benson M. Kariuki,Mohamed S. Bekheit,Yassmin Moatasim,Omnia Kutkat,Walid Fayad,May A. El-Manawaty,Ahmed A. Soliman,Riham A. El-Shiekh,Aladdin M. Srour,Reham F. Barghash,Adel S. Girgis +13 more
TL;DR: In this paper , a series of 1-alkylsulfonyl dispiro[indoline-3,2'-pyrrolidine-3',3″-piperidine]-2,4″-diones 6a'o has been synthesized through regioselective multi-component azomethine dipolar cycloaddition reaction of 1-(alkyl sulfonyls)-3,5-bis(ylidene)-piperidin-4-ones 3a'h. X-ray diffraction studies (6b'd,h) confirmed the structures.
Journal ArticleDOI
Development of spiro-3-indolin-2-one containing compounds of antiproliferative and anti-SARS-CoV-2 properties
Nehmedo G. Fawazy,Siva S. Panda,Ahmed Mostafa,Benson M. Kariuki,Mohamed S. Bekheit,Yassmin Moatasim,Omnia Kutkat,Walid Fayad,May A. El-Manawaty,Ahmed A. Soliman,Riham A. El-Shiekh,Aladdin M. Srour,Reham F. Barghash,Adel S. Girgis +13 more
TL;DR: In this article , a series of 1-alkylsulfonyl dispiro[indoline-3,2'-pyrrolidine-3',3″-piperidine]-2,4″-diones 6a'o has been synthesized through regioselective multi-component azomethine dipolar cycloaddition reaction of 1-(alkyl sulfonyls)-3,5-bis(ylidene)-piperidin-4-ones 3a'h. X-ray diffraction studies (6b'd,h) confirmed the structures.
References
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Journal ArticleDOI
Exploration of a library of triazolothiadiazole and triazolothiadiazine compounds as a highly potent and selective family of cholinesterase and monoamine oxidase inhibitors: design, synthesis, X-ray diffraction analysis and molecular docking studies
Imtiaz Khan,Syeda Mahwish Bakht,Aliya Ibrar,Saba Abbas,Shahid Hameed,Jonathan M. White,Usman Ali Rana,Sumera Zaib,Mohammad Shahid,Jamshed Iqbal +9 more
TL;DR: A diverse library of new triazolothiadiazole (4a–l) and triazolate (5a–p) compounds was designed, synthesized and evaluated as potent and selective inhibitors of electric eel acetylcholinesterase (EeAChE) and horse serum butyrylcholinease (hBChE), using Ellman's method.
Journal ArticleDOI
Combustion synthesized WO3–ZrO2 nanocomposites as catalyst for the solvent-free synthesis of coumarins
TL;DR: In this article, a mixture of tetragonal and monoclinic phases in the synthesized ZrO 2 particles were characterized by X-ray diffraction, infrared spectroscopy and transmission electron microscopy.
Journal ArticleDOI
Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.
Sahar Mohammad Bagheri,Sahar Mohammad Bagheri,Mehdi Khoobi,Hamid Nadri,Alireza Moradi,Saeed Emami,Leili Jalili-Baleh,Farnaz Jafarpour,Farshad Homayouni Moghadam,Alireza Foroumadi,Abbas Shafiee +10 more
TL;DR: A series of 4‐hydroxycoumarin‐derived compounds 8a‐p containing N‐benzyl‐1,2,3‐triazole motif were designed as A ChE inhibitors and 2‐chlorobenzyl derivative 8k showed the most potent activity against AChE.
Journal ArticleDOI
Current Acetylcholinesterase-Inhibitors: A Neuroinformatics Perspective
Sibhghatulla Shaikh,Anupriya Verma,Saimeen Siddiqui,Syed Sayeed Ahmad,Syed Mohd Danish Rizvi,Shazi Shakil,Deboshree Biswas,Divya Singh,Mohmmad H. Siddiqui,Shahnawaz Shakil,Shams Tabrez,Mohammad Amjad Kamal +11 more
TL;DR: This review presents a concise update on the inhibitors of the neuroenzyme, acetylcholinesterase (AChE; EC 3.1.7), and current status of therapeutic applications of AChEinhibitors has been summarized.
Journal ArticleDOI
Synthesis and pharmacological evaluation of donepezil-based agents as new cholinesterase/monoamine oxidase inhibitors for the potential application against Alzheimer’s disease
Fan Li,Zhi-Min Wang,Jia-Jia Wu,Jin Wang,Sai-Sai Xie,Jin-Shuai Lan,Wei Xu,Ling-Yi Kong,Xiao-Bing Wang +8 more
TL;DR: W18 was a promising agent with balanced activities, which exhibited a moderate cholinesterase inhibition and an acceptable inhibitory activity against monoamine oxidases and could also be a metal-chelator, and able to cross the blood–brain barrier with low cell toxicity on PC12 cells.