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Article

Isatin Bis-Indole and Bis-Imidazothiazole Hybrids: Synthesis and Antimicrobial Activity

by
Francesca Bonvicini
1,
Alessandra Locatelli
2,*,
Rita Morigi
2,
Alberto Leoni
2,† and
Giovanna Angela Gentilomi
1,3,†
1
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Massarenti 9, 40138 Bologna, Italy
2
Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126 Bologna, Italy
3
Division of Microbiology, IRCCS Azienda Ospedaliero-Universitaria di Bologna, Via Massarenti 9, 40138 Bologna, Italy
*
Author to whom correspondence should be addressed.
†
These authors contributed equally to this work.
Molecules 2022, 27(18), 5781; https://doi.org/10.3390/molecules27185781
Submission received: 25 July 2022 / Revised: 30 August 2022 / Accepted: 5 September 2022 / Published: 7 September 2022
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Isatin and its derivatives are important heterocycles found in nature and present in numerous bioactive compounds which possess various biological activities. Moreover, it is an essential building block in organic synthesis. The discovery of novel compounds active against human pathogenic bacteria and fungi is an urgent need, and the isatin may represent the suitable scaffold in the design of biologically relevant antimicrobials. A small library of 18 isatin hybrids was synthetized and evaluated for their antimicrobial potential on three reference strains: S. aureus, E. coli, both important human pathogens infamous for causing community- and hospital-acquired severe systemic infections; and C. albicans, responsible for devastating invasive infections, mainly in immunocompromised individuals. The study highlighted two lead compounds, 6k and 6m, endowed with inhibitory activity against S. aureus at very low concentrations (39.12 and 24.83 µg/mL, respectively).
Keywords: isatin; indole; imidazo[2,1-b]thiazole; antimicrobial agents; cytotoxicity isatin; indole; imidazo[2,1-b]thiazole; antimicrobial agents; cytotoxicity

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MDPI and ACS Style

Bonvicini, F.; Locatelli, A.; Morigi, R.; Leoni, A.; Gentilomi, G.A. Isatin Bis-Indole and Bis-Imidazothiazole Hybrids: Synthesis and Antimicrobial Activity. Molecules 2022, 27, 5781. https://doi.org/10.3390/molecules27185781

AMA Style

Bonvicini F, Locatelli A, Morigi R, Leoni A, Gentilomi GA. Isatin Bis-Indole and Bis-Imidazothiazole Hybrids: Synthesis and Antimicrobial Activity. Molecules. 2022; 27(18):5781. https://doi.org/10.3390/molecules27185781

Chicago/Turabian Style

Bonvicini, Francesca, Alessandra Locatelli, Rita Morigi, Alberto Leoni, and Giovanna Angela Gentilomi. 2022. "Isatin Bis-Indole and Bis-Imidazothiazole Hybrids: Synthesis and Antimicrobial Activity" Molecules 27, no. 18: 5781. https://doi.org/10.3390/molecules27185781

APA Style

Bonvicini, F., Locatelli, A., Morigi, R., Leoni, A., & Gentilomi, G. A. (2022). Isatin Bis-Indole and Bis-Imidazothiazole Hybrids: Synthesis and Antimicrobial Activity. Molecules, 27(18), 5781. https://doi.org/10.3390/molecules27185781

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