Abstract
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.
Highlights
As previously described [28], the initial step for the synthesis of 2,6-disubstituted benzothiazole was the preparation of two intermediates according to a modified procedure [33]: 4-amino-3-mercaptobenzoic acid hydrochloride (3) and bis(2-amino-4-benzenesulfonamide)
The aim of the present study was to improve the activity profile of previously discovered benzimidazole-structured compounds by isosteric substitution of the base nucleus with a variously substituted benzothiazole in position 2. The synthesis of this new class of benzothiazole derivatives was aimed at identifying molecules with a multifunctional biological profile, with particular attention to pathologies affecting the skin
One of the fundamental aspects of this work concerned the ability of the molecules to provide photoprotection and to safeguard against the harmful effects induced by both direct (UVB) and indirect (UVA) exposure to UV rays
Summary
Many diseases, defined as multifactorial because they are caused by multiple genetic and environmental factors, are highly variable and heterogeneous, involving multiple organ systems, tissues and potential targets. These multifactorial diseases, which involve two or more indications and have very complex etiopathologies, include atherosclerosis, Alzheimer’s disease (AD), rheumatoid arthritis, cancer, metabolic syndrome, asthma, osteoarthritis, diabetic complications, malaria, tuberculosis, neurotrauma, various CNS disorders and multiple sclerosis—diseases that are currently treated or moderated by numerous drugs belonging to different therapeutic classes [1].
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