Antimicrobial and Anti-Oxidative Activities of 12-Arylbenzoacridines

Boonsong Wungsintaweekul(1*), Kayoko Abe(2), Rintaro Koga(3), Yoshinori Katakura(4), Kohei Torikai(5)

(1) School of Pharmacy, Walailak University, 222 Thaiburi, Thasala, Nakhon Si Thammarat 80161, Thailand
(2) Graduate School of Systems Life Sciences, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
(3) Department of Chemistry, Graduate School and Faculty of Science, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
(4) Faculty of Agriculture, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
(5) Department of Chemistry, Graduate School and Faculty of Science, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan
(*) Corresponding Author


Searching biologically active compounds has been one of the major duties of organic chemists. We previously constructed a library of synthetic 12-arylbenzoacridines and found estrogenic and anti-estrogenic agents. With taking the shot-gun approach into consideration, further exploration for bioactive species in the above library was carried out. As a result, new antibacterial agents against S. aureus (MIC = 16 μM), E. coli (MIC = 7.8 μM), E. faecalis (MIC = 0.98 μM), and A. baumannii (MIC = 31 μM) were found. Moreover, we also unveiled that some of the tested compounds exhibit cell-based anti-oxidative activity. These results clearly show a good potential of 12-arylbenzoacridines as novel pharmacophores, which is useful to establish various medicines.


benzoacridine; antibacterial; shotgun approach; antioxidant


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