Synthesis and biological evaluation of some tacrine analogs: study of the effect of the chloro substituent on the acetylcholinesterase inhibitory activity

2016 ◽  
Vol 147 (3) ◽  
pp. 539-552 ◽  
Author(s):  
Hanan M. Ragab ◽  
Hayam M. A. Ashour ◽  
Amal Galal ◽  
Asser I. Ghoneim ◽  
Hassan R. Haidar
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis and Biological Evaluation of Novel Glycosyl-Containing 1,2,4-Triazolo[3,4-b][1,3,4]Thiadiazole Derivatives as Acetylcholinesterase Inhibitors

2017 ◽  
Vol 41 (10) ◽  
pp. 571-575 ◽  
Author(s):  
Xiu-Jian Liu ◽  
Lei Wang ◽  
Long Yin ◽  
Feng-Chang Cheng ◽  
Hui-Min Sun ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitors ◽  
Biological Evaluation ◽  
Synthetic Methods ◽  
Glucosamine Hydrochloride ◽  
Acetylcholinesterase Inhibitory Activity ◽  
Important Intermediate ◽  
Thiadiazole Derivatives ◽  
Ellman’S Method ◽  
Synthesis And Biological Evaluation

An efficient protocol for the synthesis of novel glycosyl-containing 1,2,4-triazolo[3,4- b][1,3,4]thiadiazole derivatives starting from the commercially available D-glucosamine hydrochloride is described by reaction of glycosyl isothiocyanate with various aminotriazoles in DMF. Glycosyl isothiocyanate is an important intermediate and synthetic methods are discussed. The acetylcholinesterase inhibitory activity of these compounds was tested by Ellman's method. It was found that most compounds exhibited over 90% inhibition and they were subsequently evaluated for their IC50 values.

Synthesis and biological evaluation of a targeted DNA-binding transcriptional activator with HDAC8 inhibitory activity

2013 ◽  
Vol 21 (14) ◽  
pp. 4201-4209 ◽  
Author(s):  
Abhijit Saha ◽  
Ganesh N. Pandian ◽  
Shinsuke Sato ◽  
Junichi Taniguchi ◽  
Kaori Hashiya ◽  
...  
Keyword(s):  
Dna Binding ◽  
Inhibitory Activity ◽  
Transcriptional Activator ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Total synthesis and biological evaluation of seven new anti-inflammatory oxacyclododecindione-type macrolactones

2020 ◽  
Vol 18 (30) ◽  
pp. 5906-5917
Author(s):  
Carina Weber ◽  
Nina Vierengel ◽  
Thorsten Walter ◽  
Torsten Behrendt ◽  
Tobias Lucas ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Signalling Pathways ◽  
Anti Inflammatory ◽  
Synthesis And Biological Evaluation

Seven new macrolactones of the oxacyclododecindione family have been synthesized and tested for their inhibitory activity on TGF-β-inducible Smad2/3- as well as IL-4-inducible STAT6-dependent signalling pathways.

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

Design, synthesis and biological evaluation of 2-amino-N-(2-aminophenyl)thiazole-5-carboxamide derivatives as novel Bcr-Abl and histone deacetylase dual inhibitors

RSC Advances ◽  
2016 ◽  
Vol 6 (105) ◽  
pp. 103178-103184 ◽  
Author(s):  
Xin Chen ◽  
Shuang Zhao ◽  
Yichao Wu ◽  
Yadong Chen ◽  
Tao Lu ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Design Approach ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Synthesis And Biological Evaluation ◽  
Novel Design

A novel design approach: combination of Bcr-Abl and HDAC inhibitory activity in one molecule to produce dual inhibitors.

scholarly journals Design, synthesis and biological evaluation of 2,3-dihydroimidazo[1,2-c]quinazoline derivatives as novel phosphatidylinositol 3-kinase and histone deacetylase dual inhibitors

RSC Advances ◽  
2017 ◽  
Vol 7 (82) ◽  
pp. 52180-52186 ◽  
Author(s):  
Yichao Wu ◽  
Weichen Dai ◽  
Xin Chen ◽  
Aixin Geng ◽  
Yadong Chen ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Design Approach ◽  
Phosphatidylinositol 3 Kinase ◽  
Design Synthesis ◽  
Dual Inhibitors ◽  
Quinazoline Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Novel Design

A novel design approach by combination of PI3K and HDAC inhibitory activity in one molecule to produce dual inhibitors.

scholarly journals Synthesis and Biological Evaluation of New Hydrazone Derivatives of Quinoline and Their Cu(II) and Zn(II) Complexes againstMycobacterium tuberculosis

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Mustapha C. Mandewale ◽  
Bapu Thorat ◽  
Dnyaneshwar Shelke ◽  
Ramesh Yamgar
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Metal Complexes ◽  
Inhibitory Activity ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Fluorescence Properties ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A new series of quinoline hydrazone derivatives and their metal complexes have been synthesized and their biological properties have been evaluated againstMycobacterium tuberculosis(H37 RV strain). Most of the newly synthesized compounds displayed 100% inhibitory activity at a concentration of 6.25–25 μg/mL, againstMycobacterium tuberculosis. Fluorescence properties of all the synthesized compounds have been studied.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

2014 ◽  
Vol 69 (1) ◽  
Author(s):  
Saleh Nazifi Ibrahim ◽  
Farediah Ahmad
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Microplate Assay ◽  
Synthetic Compounds ◽  
Ache Inhibitory Activity ◽  
Weak Activity ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation

A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration compared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay.

Design, synthesis and biological evaluation of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives as potential BRAFV600E inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (95) ◽  
pp. 52702-52711 ◽  
Author(s):  
Ya-Juan Qin ◽  
Man Xing ◽  
Ya-Liang Zhang ◽  
Jigar A. Makawana ◽  
Ai-Qin Jiang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Methyl Benzoate ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Potent Inhibitory Activity ◽  
Benzoate Derivatives

A series of (1,3-diphenyl-1H-pyrazol-4-yl) methyl benzoate derivatives (6a–10d) were designed and synthesized and evaluated as BRAFV600 inhibitors. Among them, compound 10a showed the most potent inhibitory activity against A375, WM266.4 and BRAFV600Ein vitro with IC50 values of 1.36 μM, 0.94 μM and 0.11 μM, respectively.

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