Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates
| Autor: | Maha S. Almutairi, Mona A Alsulami, Mohamed I. Attia, Nadine M. S. Moubayed, Sarah I. Bukhari, Reem I. Al-Wabli |
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| Rok vydání: | 2021 |
| Předmět: |
Antifungal Agents
Indoles Pharmaceutical Science Microbial Sensitivity Tests Pharmacology 010402 general chemistry 01 natural sciences Article Analytical Chemistry Candida tropicalis lcsh:QD241-441 Minimum inhibitory concentration chemistry.chemical_compound Structure-Activity Relationship Pharmacokinetics lcsh:Organic chemistry Anti-Infective Agents Drug Discovery Physical and Theoretical Chemistry Candida albicans Indole test 1 2 4-triazole-3-thiol biology 010405 organic chemistry Chemistry Organic Chemistry 1 2 4-Triazole Triazoles biology.organism_classification Antimicrobial In vitro 0104 chemical sciences Anti-Bacterial Agents antibacterial indole Chemistry (miscellaneous) Molecular Medicine antifungal |
| Zdroj: | Molecules Volume 26 Issue 8 Molecules, Vol 26, Iss 2292, p 2292 (2021) |
| ISSN: | 1420-3049 |
| Popis: | 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 6a-u 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 Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans. |
| Databáze: | OpenAIRE |
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