Benzothiazole Derivatives as Multifunctional Antioxidant Agents for Skin Damage: Structure–Activity Relationship of a Scaffold Bearing a Five-Membered Ring System
Ernestine Nicaise Djuidje,
Riccardo Barbari,
Anna Baldisserotto,
Elisa Durini,
Sabrina Sciabica,
Jan Balzarini,
Sandra Liekens,
Silvia Vertuani,
Stefano Manfredini
Affiliations
Ernestine Nicaise Djuidje
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Riccardo Barbari
Department of Chemical and Pharmaceutical Sciences, University of Ferrara, Via Fossato di Mortara 17-19, 44121 Ferrara, Italy
Anna Baldisserotto
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Elisa Durini
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Sabrina Sciabica
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Jan Balzarini
Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Department of Microbiology and Immunology, KU Leuven, University of Leuven, B-3000 Leuven, Belgium
Sandra Liekens
Laboratory of Virology and Chemotherapy, Rega Institute for Medical Research, Department of Microbiology and Immunology, KU Leuven, University of Leuven, B-3000 Leuven, Belgium
Silvia Vertuani
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Stefano Manfredini
Department of Life Sciences and Biotechnology, Master Course in Cosmetic Science and Technologies, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy
Skin diseases often give multifactorial damages; therefore, the development of multifunctional compounds represents a suitable approach especially against disorders that are induced by oxidative stress. Thus, taking into account the successful results we achieved on benzimidazoles, we have devised a new series of isosteric benzothiazoles and investigated their antioxidant, photoprotective, antifungal and antiproliferative activity. Particular attention has been paid to synergistic antioxidant and photoprotective properties. For compounds 9a and 10a, a multifunctional profile was outlined, supported by an excellent filtering capacity, mainly UVB, which has higher capacities than those of the reference PBSA which is currently in the market as a UV sunscreen filter. The two compounds were also the best in terms of growth inhibition of dermatophytes and Candida albicans, and 10a also showed good antioxidant activity. Furthermore, 9a was also effective on melanoma tumor cells (SK-Mel 5), making these compounds good candidates in the development of new skin protective and preventive agents.
