Bioorganic Chemistry (2020)
Update date:2022-07-30
Topics:
Andreotti, Elisa
Baldisserotto, Anna
Balzarini, Jan
Buzzi, Raissa
Dissette, Valeria
Djuidje, Ernestine Nicaise
Liekens, Sandra
Manfredini, Stefano
Sciabica, Sabrina
Serra, Elena
Vertuani, Silvia
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 60.32percent inhibition with IC50 = 4.79 μM.
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(2020)