ChemInform Abstract: Design, Synthesis, and Biological Activities of Conformationally Restricted Analogues of Primaquine with a 1,10-Phenanthroline Framework.

ChemInform ◽  
2009 ◽  
Vol 40 (2) ◽  
Author(s):  
Cheikh Sall ◽  
Ange-Desire Yapi ◽  
Nicolas Desbois ◽  
Severine Chevalley ◽  
Jean-Michel Chezal ◽  
...  
Keyword(s):  
Biological Activities ◽  
Design Synthesis ◽  
Conformationally Restricted

Design, synthesis, and biological activities of conformationally restricted analogs of primaquine with a 1,10-phenanthroline framework

2008 ◽  
Vol 18 (16) ◽  
pp. 4666-4669 ◽  
Author(s):  
Cheikh Sall ◽  
Ange-Désiré Yapi ◽  
Nicolas Desbois ◽  
Séverine Chevalley ◽  
Jean-Michel Chezal ◽  
...  
Keyword(s):  
Biological Activities ◽  
Design Synthesis ◽  
Conformationally Restricted ◽  
Conformationally Restricted Analogs

Diamides conformationally restricted with central amino acid: design, synthesis and biological activities

2022 ◽  
Author(s):  
Rui‐Jia Chen ◽  
Cong Zhou ◽  
Le‐Feng Dong ◽  
Ting‐Ting Feng ◽  
Gang‐Ao Wang ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Activities ◽  
Design Synthesis ◽  
Conformationally Restricted

Design, Synthesis and Antifungal Activity of Novel 1-(Adamantan-1-yl) ethanone Oxime Esters

2020 ◽  
Vol 17 (5) ◽  
pp. 526-532
Author(s):  
Si Liu ◽  
Li-Zhi Niu ◽  
Yan-Hua Shi ◽  
Fu-Xian Wan ◽  
Lin Jiang
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Lead Compound ◽  
Design Synthesis ◽  
Antifungal Activities

Background: Oxime compounds, including oxime ethers and oxime esters, possess various biological activities. Many oxime ethers have been widely used in the fields of pesticides and medicines. However, oxime ethers are rarely used in the field of pesticides. Methods: We chose the excellent fungicide pyrifenox as the lead compound, integrated pyridinyl, adamantyl and benzoyl moieties into one molecule, while also designed and synthesized ten 1- (adamantan-1-yl)ethanone oxime esters containing pyridinyl moiety. Moreover, we also evaluated their preliminary antifungal activities against S. sclerotiorum and B. cinerea. Results: The target compounds were characterized by NMR, IR and HRMS. The preliminary bioactivity test showed that they exhibited some antifungal activity to S. sclerotiorum and B. cinerea, and EC50 values were in the range of 14.16-32.97 and 27.60-52.82 μg/mL, respectively. Conclusion: Some target compounds such as 3d, 3e, 3h and 3i, exhibited moderate activities against S. sclerotiorum, with EC50 values of 14.16-18.18 μg/mL.

Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones

2019 ◽  
Vol 19 (9) ◽  
pp. 1132-1140
Author(s):  
Heba A.E. Mohamed ◽  
Hossa F. Al-Shareef
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Flow Cytometric Analysis ◽  
Annexin V ◽  
Cytotoxic Activities ◽  
Significant Group ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range

Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors. Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in ethanol. Results: A novel series of hybrid 2-quinolone derivatives was designed and synthesized. The compounds structures were confirmed using different spectroscopic methods and elemental analysis. The cytotoxic activities of all the compounds were assessed against HepG2 cell line in comparison with doxorubicin as a standard drug. Conclusion: Most compounds revealed superior anti-proliferative activity than the standard. Compound 4b, is the most active compound (IC50 = 0.39mM) compared with doxorubicin (IC50 = 9.23mM). DNA flow cytometric analysis of compound 4b showed cell cycle arrest at G2/M phase with a concomitant increase of cells in apoptotic phase. Dual annexin-V/ propidium iodide staining assay of compound 4b revealed that the selected candidate increased the apoptosis of HepG-2 cells more than control.

Functional design of glycan-conjugated molecules using a chemoenzymatic approach

2021 ◽  
Author(s):  
Makoto Ogata
Keyword(s):  
Molecular Weight ◽  
Large Scale ◽  
Biological Activities ◽  
Natural Compounds ◽  
Low Molecular Weight ◽  
Functional Design ◽  
Enzymatic Method ◽  
Conjugated Molecules ◽  
Design Synthesis ◽  
And Function

Abstract Carbohydrates play important and diverse roles in the fundamental processes of life. We have established a method for accurately and a large scale synthesis of functional carbohydrates with diverse properties using a unique enzymatic method. Furthermore, various artificial glycan-conjugated molecules have been developed by adding these synthetic carbohydrates to macromolecules and to middle and low molecular weight molecules with different properties. These glycan-conjugated molecules have biological activities comparable to or higher than those of natural compounds, and present unique functions. In this review, several synthetic glycan-conjugated molecules are taken as examples to show design, synthesis and function.

Design, Synthesis and Biological Activities of Novel Anthranilic Diamide Insecticide Containing Trifluoroethyl Ether

2012 ◽  
Vol 30 (8) ◽  
pp. 1748-1758 ◽  
Author(s):  
Yu Zhao ◽  
Yongqiang Li ◽  
Lixia Xiong ◽  
Hongxue Wang ◽  
Zhengming Li
Keyword(s):  
Biological Activities ◽  
Design Synthesis ◽  
Anthranilic Diamide ◽  
Diamide Insecticide

scholarly journals Conformationally restricted benzothienoazepine respiratory syncytial virus inhibitors: their synthesis, structural analysis and biological activities

MedChemComm ◽  
2018 ◽  
Vol 9 (3) ◽  
pp. 583-589 ◽  
Author(s):  
Euan A. F. Fordyce ◽  
S. Fraser Hunt ◽  
Damien Crepin ◽  
Stuart T. Onions ◽  
Guillaume F. Parra ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Structural Analysis ◽  
Biological Activities ◽  
Bioactive Conformation ◽  
Conformationally Restricted ◽  
Syncytial Virus

Study of atropisomerism around RSV inhibitors allows identification of bioactive conformation.

Design, synthesis and photophysical aspects of 1,2,3-triazole appended schiff base functionalized silanes and silatranes

2021 ◽  
Author(s):  
Gurjaspreet Singh ◽  
Priyanka . ◽  
Sushma . ◽  
Mehta Diksha ◽  
Mohit Kalyan ◽  
...  
Keyword(s):  
Schiff Base ◽  
Biological Activities ◽  
Design Synthesis ◽  
Organosilicon Chemistry

Organosilicon chemistry is appraised as the trunk of coalescence and structural manoeuvre of moieties. Schiff base compounds are popular auxiliary scaffolds having vast applications in the fields of biological activities,...

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