Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates <b&...
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| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/8/2292 |
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| author | Reem I. Al-Wabli Mona A. Alsulami Sarah I. Bukhari Nadine M. S. Moubayed Maha S. Al-Mutairi Mohamed I. Attia |
| author_facet | Reem I. Al-Wabli Mona A. Alsulami Sarah I. Bukhari Nadine M. S. Moubayed Maha S. Al-Mutairi Mohamed I. Attia |
| author_sort | Reem I. Al-Wabli |
| collection | DOAJ |
| description | The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates <b>6a-u</b> was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against <i>Candida tropicalis</i> with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound <b>6f</b> is the most potent congener with an MIC value of 2 µg/mL against <i>Candida albicans</i>. |
| first_indexed | 2024-03-10T12:18:13Z |
| format | Article |
| id | doaj.art-41d9455c19a3453292da5ee7a681a986 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T12:18:13Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-41d9455c19a3453292da5ee7a681a9862023-11-21T15:41:44ZengMDPI AGMolecules1420-30492021-04-01268229210.3390/molecules26082292Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole ConjugatesReem I. Al-Wabli0Mona A. Alsulami1Sarah I. Bukhari2Nadine M. S. Moubayed3Maha S. Al-Mutairi4Mohamed I. Attia5Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaBotany and Microbiology Department, College of Science, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi ArabiaThe increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates <b>6a-u</b> was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against <i>Candida tropicalis</i> with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound <b>6f</b> is the most potent congener with an MIC value of 2 µg/mL against <i>Candida albicans</i>.https://www.mdpi.com/1420-3049/26/8/2292indole1,2,4-triazole-3-thiolantibacterialantifungal |
| spellingShingle | Reem I. Al-Wabli Mona A. Alsulami Sarah I. Bukhari Nadine M. S. Moubayed Maha S. Al-Mutairi Mohamed I. Attia Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates Molecules indole 1,2,4-triazole-3-thiol antibacterial antifungal |
| title | Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates |
| title_full | Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates |
| title_fullStr | Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates |
| title_full_unstemmed | Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates |
| title_short | Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates |
| title_sort | design synthesis and antimicrobial activity of certain new indole 1 2 4 triazole conjugates |
| topic | indole 1,2,4-triazole-3-thiol antibacterial antifungal |
| url | https://www.mdpi.com/1420-3049/26/8/2292 |
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