Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates

• Published in: Molecules (Basel, Switzerland) Vol. 26; no. 8; p. 2292
• Main Authors: Al-Wabli, Reem I, Alsulami, Mona A, Bukhari, Sarah I, Moubayed, Nadine M S, Al-Mutairi, Maha S, Attia, Mohamed I
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 15.04.2021; MDPI
• Subjects: 1,2,4-triazole-3-thiol; Analgesics; Anti-Bacterial Agents - chemical synthesis; Anti-Bacterial Agents - chemistry; Anti-Bacterial Agents - pharmacology; Anti-Infective Agents - chemical synthesis; Anti-Infective Agents - chemistry; Anti-Infective Agents - pharmacology; antibacterial; Antibiotics; antifungal; Antifungal Agents - chemical synthesis; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; Antimicrobial activity; Antimicrobial agents; Bacteria; Bacterial infections; Cancer; Congeners; Conjugates; Drug development; E coli; Ethanol; Evaluation; Fungicides; Gram-positive bacteria; indole; Indoles; Indoles - chemistry; Microbial Sensitivity Tests; Microorganisms; Minimum inhibitory concentration; Nosocomial infections; Pharmacodynamics; Pharmacokinetics; Pharmacology; Salmonella; Structure-Activity Relationship; Sulfur; Triazoles; Triazoles - chemical synthesis; Triazoles - chemistry; Triazoles - pharmacology; Tropical diseases; Tuberculosis; antifungal; antibacterial; 1,2,4-triazole-3-thiol; indole
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules26082292

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 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 with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound is the most potent congener with an MIC value of 2 µg/mL against .