engleski

Synthesis of novel 2-arylbenzothiazole derivatives and biological evaluation of antioxidant, antibacterial and antitumor activity

Studies of benzothiazole derivatives became a rapidly developing and increasingly active field due to their interesting pharmacological properties. Benzothiazole analogues offer a high degree of structural diversity that is useful in search of new therapeutic agents [1]. In connection with our previous studies focused on synthesis and antitumor activity of 2- arylbenzothiazole derivatives [2-4] we now put our attention on the synthesis of a series of novel 2-hydroxyphenyl- and 2- methoxyphenylbenzothiazole compounds (Figure 1). Different substituents at 6-position of the benzothiazole skeleton were introduced through condensation reactions involving 5-substituted- 2-aminothiphenols and the corresponding benzaldehydes. Antiproliferative effects of compounds 1-12 were evaluated on a panel of tumor cell lines in vitro and normal human fibroblasts. Antibacterial properties were determined against two G+ and two G- bacterial strains. In addition, in vitro antioxidant potencies were measured by use of DPPH, FRAP and ABTS tests. Preliminary structure-activity relationships for synthesized compounds are presented herein.

2-arylbenzothiazole, biological evaluation

nije evidentirano