Regioselective One-Pot Synthesis, Biological Activity and Molecular Docking Studies of Novel Conjugates <i>N</i>-(p-Aryltriazolyl)-1,5-benzodiazepin-2-ones as Potent Antibacterial and Antifungal Agents
Asma Nsira,
Hasan Mtiraoui,
Sami Chniti,
Hanan Al-Ghulikah,
Rafik Gharbi,
Moncef Msaddek
Affiliations
Asma Nsira
Laboratory of Heterocyclic Chemistry Natural Products and Reactivity/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia
Hasan Mtiraoui
Laboratory of Heterocyclic Chemistry Natural Products and Reactivity/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia
Sami Chniti
Laboratory of Heterocyclic Chemistry Natural Products and Reactivity/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia
Hanan Al-Ghulikah
Department of Chemistry, College of Sciences, Princess Nourah bint Abdulrahman University, P.O. Box 84428, Riyadh 11671, Saudi Arabia
Rafik Gharbi
Laboratory of Applied Chemistry and Environment, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia
Moncef Msaddek
Laboratory of Heterocyclic Chemistry Natural Products and Reactivity/CHPNR, Department of Chemistry, Faculty of Science of Monastir, University of Monastir, Monastir 5000, Tunisia
Novel 1,2,3-triazolo-linked-1,5-benzodiazepinones were designed and synthesized via a Cu(I)-catalyzed 1,3-dipolar alkyne-azide coupling reaction (CuAAC). The chemical structures of these compounds were confirmed by 1H NMR, 13C NMR, HMBC, HRMS, and elemental analysis. The compounds were screened for their in vitro antibacterial and antifungal activities. Several compounds exhibited good to moderate activities compared to those of established standard drugs. Furthermore, the binding interactions of these active analogs were confirmed through molecular docking.
