Design, synthesis, antifungal activity, and 3D-QSAR of coumarin derivatives

Novel pyrrolidine-2,4-dione derivatives were designed based on natural products. Some synthesized compounds showed excellent antifungal activity. Scanning electron microscopy was used to observe mycelium morphology. 3D-QSAR was also studied.

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Design, synthesis, antifungal activity and 3D-QSAR study of novel pyrazole carboxamide and niacinamide derivatives containing benzimidazole moiety

New Journal of Chemistry ◽

10.1039/c8nj05150j ◽

2019 ◽

Vol 43 (7) ◽

pp. 3000-3010 ◽

Cited By ~ 10

Author(s):

Wei-Jie Si ◽

Xiao-Bin Wang ◽

Min Chen ◽

Meng-Qi Wang ◽

Ai-Min Lu ◽

...

Keyword(s):

Antifungal Activity ◽

Predictive Ability ◽

3D Qsar ◽

Qsar Model ◽

Qsar Study ◽

Design Synthesis ◽

Effective Inhibition

The synthesized pyrazole carboxamide and niacinamide derivatives containing a benzimidazole moiety showed effective inhibition of the fungus B. cinereal growth. The 3D-QSAR model was built and revealed fine predictive ability.

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Synthesis and Antifungal Activity of Coumarins Derivatives Against Sporothrix spp.

Current Topics in Medicinal Chemistry ◽

10.2174/1568026618666180221115508 ◽

2018 ◽

Vol 18 (2) ◽

pp. 164-171 ◽

Cited By ~ 4

Author(s):

Luana da S.M. Forezi ◽

Luana Pereira Borba-Santos ◽

Mariana F.C. Cardoso ◽

Vitor F. Ferreira ◽

Sonia Rozental ◽

...

Keyword(s):

Antifungal Activity ◽

Antifungal Agents ◽

Sporothrix Schenckii ◽

Public Health Problem ◽

Domestic Animals ◽

Coumarin Derivatives ◽

Sporothrix Brasiliensis ◽

Synthetic Routes ◽

Effective Drugs

Sporotrichosis is a serious public health problem in Brazil that affects human patients and domestic animals, mainly cats. Thus, the search for new antifungal agents is required also due to the emergence and to the lack of effective drugs available in the therapeutic arsenal. The aim of this study was to evaluate the in vitro antifungal profile of two synthetic series of coumarin derivatives against Sporothrix schenckii and Sporothrix brasiliensis. The three-components synthetic routes used for the preparation of coumarin derivatives have proved to be quite efficient and compounds 16 and 17 have been prepared in good yields. The inhibitory activity of nineteen synthetic coumarins derivatives 16a-i and 17a-j were evaluated against Sporothrix spp. yeasts and the most potent compounds were 16b and 17i. However, according to concentrations able to inhibit (minimum inhibitory concentrations) and kill (minimum fungicidal concentrations) the cells, 17i was more effective than 16b against Sporothrix spp. Thus, 17i exhibited good antifungal activity against S. brasiliensis and S. schenckii, suggesting that it is an important scaffold for the development of novel antifungal agents.

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

Letters in Drug Design & Discovery ◽

10.2174/1570180816666190329225307 ◽

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.

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Design, Synthesis and Biological Evaluation of Some New Coumarin Derivatives as Potential Antimicrobial Agents

Medicinal Chemistry ◽

10.2174/1573406410666140902110452 ◽

2015 ◽

Vol 11 (2) ◽

pp. 128-134 ◽

Cited By ~ 14

Author(s):

Lav Kumar Singh ◽

Priyanka ◽

Vineeta Singh ◽

Diksha Katiyar

Keyword(s):

Antimicrobial Agents ◽

Biological Evaluation ◽

Coumarin Derivatives ◽

Design Synthesis ◽

Synthesis And Biological Evaluation

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Streptochlorin analogues as potential antifungal agents: Design, synthesis, antifungal activity and molecular docking study

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2021.116073 ◽

2021 ◽

Vol 35 ◽

pp. 116073

Author(s):

Ya Gao ◽

Dai-Chuan Huang ◽

Chang Liu ◽

Zi-Long Song ◽

Jing-Rui Liu ◽

...

Keyword(s):

Molecular Docking ◽

Antifungal Activity ◽

Antifungal Agents ◽

Docking Study ◽

Molecular Docking Study ◽

Design Synthesis

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7-Alkoxy-appended coumarin derivatives: synthesis, photo-physical properties, aggregation behaviours and current–voltage (I–V) characteristic studies on thin films

RSC Advances ◽

10.1039/d1ra00762a ◽

2021 ◽

Vol 11 (17) ◽

pp. 10212-10223

Author(s):

Abhijit Rudra Paul ◽

Bapi Dey ◽

Sudip Suklabaidya ◽

Syed Arshad Hussain ◽

Swapan Majumdar

Keyword(s):

Thin Films ◽

Carboxylic Acid ◽

Physical Properties ◽

Chemical Characteristics ◽

Coumarin Derivatives ◽

Design Synthesis ◽

Electrical Switching ◽

Physico Chemical ◽

Current Voltage

In this article, we demonstrate the design, synthesis and physico-chemical characteristics, including electrical switching behaviours of long alkoxy-appended coumarin carboxylate/carboxylic acid in thin films.

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