Oxidative stress is the product or aetiology of various multifactorial diseases; on the other hand, the development of multifunctional compounds is a recognized strategy for the control of complex diseases. To this end, a series of benzothiazole derivatives was synthesized and evaluated for their multifunctional effectiveness as antioxidant, sunscreen (filter), antifungal and antiproliferative agents. Compounds were easily synthesized via condensation reaction between 2-aminothiophenols and different benzaldehydes. SAR study, particularly in position 2 and 6 of benzothiazoles, led to the identification of 4g and 4k as very interesting potential compounds for the design of multifunctional drugs. In particular, compound 4g is the best blocker of hERG potassium channels expressed in HEK 293 cells exhibiting 60.32% inhibition with IC50 = 4.79 μM.

Design, synthesis and evaluation of benzothiazole derivatives as multifunctional agents

Djuidje E. N.
Primo
;
Sciabica S.;Buzzi R.;Dissette V.;Serra E.;Manfredini S.;Vertuani S.
Penultimo
;
Baldisserotto A.
Ultimo
2020

Abstract

Oxidative stress is the product or aetiology of various multifactorial diseases; on the other hand, the development of multifunctional compounds is a recognized strategy for the control of complex diseases. To this end, a series of benzothiazole derivatives was synthesized and evaluated for their multifunctional effectiveness as antioxidant, sunscreen (filter), antifungal and antiproliferative agents. Compounds were easily synthesized via condensation reaction between 2-aminothiophenols and different benzaldehydes. SAR study, particularly in position 2 and 6 of benzothiazoles, led to the identification of 4g and 4k as very interesting potential compounds for the design of multifunctional drugs. In particular, compound 4g is the best blocker of hERG potassium channels expressed in HEK 293 cells exhibiting 60.32% inhibition with IC50 = 4.79 μM.
2020
Djuidje, E. N.; Sciabica, S.; Buzzi, R.; Dissette, V.; Balzarini, J.; Liekens, S.; Serra, E.; Andreotti, E.; Manfredini, S.; Vertuani, S.; Baldisserotto, A.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11392/2427822
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