Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening
Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present...
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MDPI AG
2021-01-01
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| Series: | Applied Sciences |
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| Online Access: | https://www.mdpi.com/2076-3417/11/3/1180 |
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| author | Kinga Paruch Łukasz Popiołek Anna Biernasiuk Anna Berecka-Rycerz Anna Malm Anna Gumieniczek Monika Wujec |
| author_facet | Kinga Paruch Łukasz Popiołek Anna Biernasiuk Anna Berecka-Rycerz Anna Malm Anna Gumieniczek Monika Wujec |
| author_sort | Kinga Paruch |
| collection | DOAJ |
| description | Bacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound <b>15</b>, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL. |
| first_indexed | 2024-03-09T03:30:12Z |
| format | Article |
| id | doaj.art-18104a9c0d1640d2a1285bafc19f0c7b |
| institution | Directory Open Access Journal |
| issn | 2076-3417 |
| language | English |
| last_indexed | 2024-03-09T03:30:12Z |
| publishDate | 2021-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Applied Sciences |
| spelling | doaj.art-18104a9c0d1640d2a1285bafc19f0c7b2023-12-03T14:56:28ZengMDPI AGApplied Sciences2076-34172021-01-01113118010.3390/app11031180Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity ScreeningKinga Paruch0Łukasz Popiołek1Anna Biernasiuk2Anna Berecka-Rycerz3Anna Malm4Anna Gumieniczek5Monika Wujec6Chair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, PolandChair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, PolandChair and Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Lublin, 1 Chodźki Street, 20-093 Lublin, PolandChair and Department of Medicinal Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4 Jaczewskiego Street, 20-093 Lublin, PolandChair and Department of Pharmaceutical Microbiology, Faculty of Pharmacy, Medical University of Lublin, 1 Chodźki Street, 20-093 Lublin, PolandChair and Department of Medicinal Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4 Jaczewskiego Street, 20-093 Lublin, PolandChair and Department of Organic Chemistry, Faculty of Pharmacy, Medical University of Lublin, 4A Chodźki Street, 20-093 Lublin, PolandBacterial infections, especially those caused by strains resistant to commonly used antibiotics and chemotherapeutics, are still a current threat to public health. Therefore, the search for new molecules with potential antimicrobial activity is an important research goal. In this article, we present the synthesis and evaluation of the in vitro antimicrobial activity of a series of 15 new derivatives of 4-methyl-1,2,3-thiadiazole-5-carboxylic acid. The potential antimicrobial effect of the new compounds was observed mainly against Gram-positive bacteria. Compound <b>15</b>, with the 5-nitro-2-furoyl moiety, showed the highest bioactivity: minimum inhibitory concentration (MIC) = 1.95–15.62 µg/mL and minimum bactericidal concentration (MBC)/MIC = 1–4 µg/mL.https://www.mdpi.com/2076-3417/11/3/11801,2,3-thiadiazole derivativesantimicrobial activityhydrazide–hydrazoneslipophilicityorganic synthesis |
| spellingShingle | Kinga Paruch Łukasz Popiołek Anna Biernasiuk Anna Berecka-Rycerz Anna Malm Anna Gumieniczek Monika Wujec Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening Applied Sciences 1,2,3-thiadiazole derivatives antimicrobial activity hydrazide–hydrazones lipophilicity organic synthesis |
| title | Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening |
| title_full | Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening |
| title_fullStr | Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening |
| title_full_unstemmed | Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening |
| title_short | Novel Derivatives of 4-Methyl-1,2,3-Thiadiazole-5-Carboxylic Acid Hydrazide: Synthesis, Lipophilicity, and In Vitro Antimicrobial Activity Screening |
| title_sort | novel derivatives of 4 methyl 1 2 3 thiadiazole 5 carboxylic acid hydrazide synthesis lipophilicity and in vitro antimicrobial activity screening |
| topic | 1,2,3-thiadiazole derivatives antimicrobial activity hydrazide–hydrazones lipophilicity organic synthesis |
| url | https://www.mdpi.com/2076-3417/11/3/1180 |
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