Design, Synthesis and Antifungal Activity of the Novel Water-Soluble Prodrug of Antifungal Triazole CS-758

The novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones (4a-j) analogs were synthesized by Knoevenagel condensation of a solution of 2-methyl-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4-dihydro-4-quinazolinone (3) with aromatic aldehyde in presence of catalytic amount of piperidine. Compounds (4a-j) showed significant biological activity against all the standard strains. All the synthesized compounds were characterized on the basis of their IR,1H NMR, MASS spectroscopic data and elemental analyses. All the compounds have been tested for antimicrobial and antifungal activity by the cup-plate method.

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Design, Synthesis and Antifungal Activity of a Novel Water Soluble Prodrug (I) of Antifungal Triazole.

ChemInform ◽

10.1002/chin.200317111 ◽

2003 ◽

Vol 34 (17) ◽

Author(s):

Isao Umeda ◽

et al. et al.

Keyword(s):

Antifungal Activity ◽

Water Soluble ◽

Design Synthesis

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Self Microemulsifying Nutraceutical and Drug Delivery Systems

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.3.3 ◽

2014 ◽

Vol 7 (3) ◽

pp. 2520-2528 ◽

Cited By ~ 1

Author(s):

Vikrant P Wankhade ◽

Nivedita S Kale ◽

K.K Tapar

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Ternary Phase Diagram ◽

Aqueous Solubility ◽

Oral Formulation ◽

Water Soluble ◽

Drug Dissolution ◽

The Novel ◽

Peristaltic Movement

Many chemical entities and nutraceuticals are poor water soluble and show high lipophilicity. It’s difficult to formulate them into oral formulation because of its low aqueous solubility which ultimately affects bioavailability. To enhance the bioavailability of such drugs compounds, self microemulsifying drug delivery system is the reliable drug delivery system. In this system the drug is incorporated in the isotropic system and formulated as unit dosage form. Self microemulsifying drug delivery system is the novel emulsified system composed of anhydrous isotropic mixture of oils, surfactant, and co solvent and sometimes co surfactant. Drug is directly dispersed into the entire gastro intestinal tract with continuous peristaltic movement and drug is available in the solution form of microemulsion, absorbed through lymphatic system and bypasses the dissolution step. Hence they increase the patient compliance. The excipients are selected on basis of construction of ternary phase diagram. Self micro-emulsifying drug delivery system is very useful for drug in which drug dissolution is rate limiting step. This review describes the novel approaches and evaluation parameters of the self microemulsifying drug delivery system towards different classic drugs, proteins-peptides, and nutraceuticals in various oral microemulsion compositions and microstructures.

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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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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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Design, Synthesis and Evaluate In Vitro Antifungal Activity of Novel Benzamide Derivatives

Journal of the chemical society of pakistan ◽

10.52568/000763/jcsp/41.03.2019 ◽

2019 ◽

Vol 41 (3) ◽

pp. 549-549

Author(s):

Xuesong Wang and Xiaorong Tang Xuesong Wang and Xiaorong Tang

Keyword(s):

Antifungal Activity ◽

Pathogenic Fungi ◽

Gibberella Zeae ◽

Design Synthesis ◽

Carboxylic Acid Amides ◽

Almost All ◽

Negative Controls ◽

New Compounds ◽

Benzamide Derivatives

A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together. The antifungal activity of the 15 new compounds were evaluated in vitro against five pathogenic fungi, including Sclerotinia sclerotiorum, Gibberella zeae, Rhizoctonia solani, Helminthosporium maydis and Botrytis cinerea. Almost all the structure have not been reported, except compounds 3, 5 and 6. A surprising finding is that all the five tested fungi breed faster than negative controls when supplementary with compound 715 , respectively.

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