Benzothiazole Derivatives as Multifunctional Antioxidant Agents for Skin Damage: Structure-Activity Relationship of a Scaffold Bearing a Five-Membered Ring System

• Main Authors: Ernestine Nicaise Djuidje (Author), Riccardo Barbari (Author), Anna Baldisserotto (Author), Elisa Durini (Author), Sabrina Sciabica (Author), Jan Balzarini (Author), Sandra Liekens (Author), Silvia Vertuani (Author), Stefano Manfredini (Author)
• Format: Book
• Published: MDPI AG, 2022-02-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/antiox11020407; 2076-3921
• Keywords: benzothiazole; multifunctional; UV filter; antioxidant; antimicrobial; cosmeceutical; Therapeutics. Pharmacology; RM1-950
• Source: Antioxidants, Vol 11, Iss 2, p 407 (2022)

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 <b>9a</b> and <b>10a</b>, 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 <b>10a</b> also showed good antioxidant activity. Furthermore, <b>9a</b> 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.