scholarly journals Design, Synthesis and Fungicidal Activity of Novel (E)-Methyl 2-{2-[(coumarin-7-yloxy)methyl]phenyl}-3-methoxyacrylates

2007 ◽  
Vol 2 (8) ◽  
pp. 1934578X0700200
Author(s):  
Chang-Ling Liu ◽  
Miao Li ◽  
Ai-Ying Guan ◽  
Hong Zhang ◽  
Zheng-Ming Li
Keyword(s):  
Downy Mildew ◽  
Fungicidal Activity ◽  
Biological Activities ◽  
Design Synthesis ◽  
Cucumber Downy Mildew ◽  
Coumarin 7 ◽  
Methyl Phenyl

A number of 7-hydroxycoumarins (5), on treatment with one equivalent of ( E)-methyl 2-{2-[(chloromethyl)phenyl]}-3-methoxyacrylate (6) at 80°C for 6–8 h, afforded ( E)-methyl 2-{2-[(coumarin-7-yloxy)methyl]phenyl}-3-methoxyacrylates (2) in 80–85% yields. The 7-hydroxycoumarins (5) were in turn prepared from resorcinols (3) and substituted ethyl 3-oxopropanoate (4). Subsequently, results of biological activities evaluated in the greenhouse indicated that several of these compounds have good fungicidal activity against cucumber downy mildew (CDM) at 25g ai/ha.

scholarly journals Synthesis and Bioactivity of Novel Coumarin Derivatives

2011 ◽  
Vol 6 (12) ◽  
pp. 1934578X1100601
Author(s):  
Ai-Ying Guan ◽  
Chang-Ling Liu ◽  
Miao Li, Zhi-Nian Li ◽  
Ming-Xing Zhang ◽  
Hong Zhang
Keyword(s):  
Powdery Mildew ◽  
Fungicidal Activity ◽  
Optimal Structure ◽  
Test Results ◽  
Coumarin Derivatives ◽  
Keto Esters ◽  
Wheat Powdery Mildew ◽  
Grey Mold ◽  
Coumarin 7 ◽  
Methyl Phenyl

A series of coumarin derivatives (6-8) containing ( E)-methyl 2-(methoxyimino)-2-phenylacetate, ( E)-2-(methoxyimino )-N-methyl-2-phenylacetamide and methyl methoxy(phenyl)carbamate were synthesized from substituted resorcinols (1) and substituted β-keto esters (2) as starting material via cyclization and condensation reactions. The test results indicated that ( E)-methyl 2-{2-[(3-hexyl-4-methyl-coumarin-7-yloxy)methyl]phenyl}-2-(methoxyimino)acetate (6f) was the optimal structure with good fungicidal activity against cucumber grey mold (CGM) giving 100% control at 100 mg L−1 concentration, much higher than that of coumoxystrobin. Methyl 2-[(3,4-dimethyl-coumarin -7-yloxy)methyl]phenyl(methoxy)carbamate (8a) was another optimal structure with good fungicidal activity against wheat powdery mildew (WPM) showing 100% control at 50 mg L−1 concentration, at the same level as that of the commercial kresoxim-methyl, and very significantly higher than that of coumoxystrobin (no control against WPM at 400 mg L−1).

scholarly journals Design, Synthesis and Biological Activity of New Strobilurin Derivatives with a 1H-Pyrazol-5-oxy Side Chain

2009 ◽  
Vol 4 (9) ◽  
pp. 1934578X0900400 ◽  
Author(s):  
Miao Li ◽  
Chang-Ling Liu ◽  
Ji-Chun Yang ◽  
Lin Li ◽  
Zhi-Nian Li ◽  
...  
Keyword(s):  
Biological Activity ◽  
Powdery Mildew ◽  
Fungicidal Activity ◽  
Green Peach Aphid ◽  
Biological Evaluation ◽  
Side Chain ◽  
Design Synthesis ◽  
H Nmr ◽  
Elemental Analyses ◽  
Cucumber Downy Mildew

A series of new strobilurin derivatives with a substituted pyrazole side chain (5 and 6) were designed and synthesized. The new derivatives were synthesized from substituted phenones as starting material via esterification, cyclization and condensation reactions. All compounds were identified by 1H NMR and IR spectral and elemental analyses. Preliminary biological evaluation showed that some of the compounds had good fungicidal activity against cucumber downy mildew (CDM) and wheat powdery mildew (WPM) at 6.25 and 1.56 mg L−1, respectively. Some of the compounds showed insecticidal activity against armyworm (AW), green peach aphid (GPA) and culex mosquitoes at 600 mg L−1.

scholarly journals Design, Synthesis and Fungicidal Activity of Novel Strobilurin Analogues Containing Substituted N-phenylpyrimidin-2-amines

2009 ◽  
Vol 4 (9) ◽  
pp. 1934578X0900400
Author(s):  
Hui-Chao Li ◽  
Chang-Ling Liu ◽  
Bao-Shan Chai ◽  
Miao Li ◽  
Zhi-Nian Li ◽  
...  
Keyword(s):  
Biological Activity ◽  
Fungicidal Activity ◽  
Biological Activities ◽  
Design Synthesis ◽  
Strobilurin Fungicide ◽  
New Compounds

A series of novel compounds (5-8) was designed and synthesized by integrating the active pharmacophore of the N-phenylpyrimidin-2-amine fungicide with the structure of strobilurin fungicide. The rationale of this approach was to determine if these new compounds exhibit unique biological activity (selectivity and potency) compared with the commercial standards. The title compounds were prepared from 2-(phenylamino)pyrimidin-4-ols (3) by treatment with one equivalent of intermediates (4) containing strobilurin pharmacophores. 2-(Phenylamino)pyrimidin-4-ols (3) were in turn prepared from phenylguanidines (1) and substituted β-ketoesters (2). Biological activities evaluated in the greenhouse indicated that compounds 5a, 6a and 7a have good fungicidal activity at 25 mg/L, comparable with that of the commercial standards, cyprodinil and azoxystrobin.

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.

Management of Dermatophytoses by Foliose Lichen; Heterodermia diademata (Taylor) D.D. Awasthi

2017 ◽  
Vol 5 (2) ◽  
pp. 79-84
Author(s):  
Anand Pandey ◽  
◽  
Awadhesh Kumar ◽  
Anupam Dikshit ◽  
◽  
...  
Keyword(s):  
Fungicidal Activity ◽  
Trichophyton Rubrum ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Ethanolic Extract ◽  
Microsporum Gypseum ◽  
Superficial Infection ◽  
Recent Advancement ◽  
Secondary Substances ◽  
Foliose Lichen

Lichens are demarcated as an association of two distinct and dissimilar components; the mycobiont (a fungus) and the phycobionts (an alga) forming a composite organism. The recent advancement in science has paid much attention on the biological roles of lichen secondary substances; which are attributed with a lot of biological activities, such as antibacterial, antifungal, antiviral, anti-inflammatory, anti-tumor, and antioxidant activities. The current research aims to unravel the fungicidal activity of lichen Heterodermia diademata, ethanolic extract (HDE) against prevalent superficial infection causing dermatophytes viz., Trichophyton rubrum, T. mentagrophytes, Microsporum gypseum and M. canis. The HDE was found active against M. gypseum and T. mentagrophytes with MIC; 1.68 and 1.98 mg/ml and mg/ml respectively. The dermatophytes were also analyzed by molecular phylogeny of chs-1 gene for variability in MIC and prediction of susceptible pathogens.

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 Fungicidal Activity of Novel Analogues of Pyrrolnitrin

2009 ◽  
Vol 57 (17) ◽  
pp. 7912-7918 ◽  
Author(s):  
Ming-Zhong Wang ◽  
Han Xu ◽  
Qi Feng ◽  
Li-Zhong Wang ◽  
Su-Hua Wang ◽  
...  
Keyword(s):  
Fungicidal Activity ◽  
Design Synthesis
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