Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity

One of the most serious future challenges to health care professionals is the emergence of multi-drug resistance pathogenic microbes that rapidly develop resistance to currently used antibiotics. So, as a way to overcome the antimicrobial drug-resistance problems, it is urgent need to synthesize several new lead molecules that are expected to have antibacterial and antifungal activities. So, some new thiazolidinone and methylthiazole derivatives incorporating benzodioxole nucleolus were constructed. Two different series of <i>N</i>-substituted thiosemicarbazones carrying a benzodioxole nucleus were synthesized through mutation reaction of the different aromatic and heterocyclic aldehydes with benzodioxolyl thiosemicarbazide. Cycloalkylation reaction of the latter thiosemicarbazones through with both of the ethyl chloroacetate or chloroacetone gave the thiazolidin-4-ones or 4-methylthiazoles, respectively. The antimicrobial activity of the thiazolidin-4-one and 4-methylthiazole derivatives was investigated. All of compounds showed from weak to moderate effects toward all tested bacteria.

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Publication Details

Journal
Synthetic Communications
Published
2024-08-09
DOI
https://doi.org/10.1080/00397911.2024.2387118
Citations
4
Primary Topic
Synthesis and biological activity
Type
article
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1.00
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article

Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity

Reem Alharbi
4 citations
Synthetic Communications
Synthesis and biological activity
1.00
article

Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity

Reem Alharbi
article en
4 citations

Abstract

One of the most serious future challenges to health care professionals is the emergence of multi-drug resistance pathogenic microbes that rapidly develop resistance to currently used antibiotics. So, as a way to overcome the antimicrobial drug-resistance problems, it is urgent need to synthesize several new lead molecules that are expected to have antibacterial and antifungal activities. So, some new thiazolidinone and methylthiazole derivatives incorporating benzodioxole nucleolus were constructed. Two different series of <i>N</i>-substituted thiosemicarbazones carrying a benzodioxole nucleus were synthesized through mutation reaction of the different aromatic and heterocyclic aldehydes with benzodioxolyl thiosemicarbazide. Cycloalkylation reaction of the latter thiosemicarbazones through with both of the ethyl chloroacetate or chloroacetone gave the thiazolidin-4-ones or 4-methylthiazoles, respectively. The antimicrobial activity of the thiazolidin-4-one and 4-methylthiazole derivatives was investigated. All of compounds showed from weak to moderate effects toward all tested bacteria.

Synthetic CommunicationsVol. 54(16)
Taibah University (SA)
Openalex Percentile: Top 27%
Synthesis and biological activity
1.00
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Synthesis of thiazolidinone and methylthiazole derivatives incorporating benzodioxole moiety and evaluation of their antimicrobial activity — Reem Alharbi · Synthetic Communications (2024) | TGRS Research Map | TGRS