Novel activities of 1-adamantylthiopyridines as antibacterials, antimalarials and anticancers

Abstract

To discover new bioactive lead compounds for medicinal purposes, herein, 2(1adamantylthio)pyridine and derivatives (1-10) were prepared and tested for antibacterial (agar dilution method against 27 strains of microorganisms), antimalarial (against Plasmodium falciparum) and anticancer (MOLT-3, HepG2, HuCCA-1 and A549) activities. Results showed that all the tested derivatives selectively exerted antigrowth activity against Streptococci at 15-30 μg/mL. 3-Substituted (R) thiopyridines; 3 (R = NAc2), 5 (R = OH) and 6 (R = Br) exhibited antibacterials, antimalarials and anticancers. Significantly, 6-(1-adamantylthio) nicotinonitrile (10) is a promising antibacterial which selectively displays antigrowth activity against Vibrio cholerae, Vibrio parahaemolyticus, Edwardsiella tarda and β-hemolytic Streptococcus group A with minimum inhibitory concentration of 30 μg/mL. The findings reveal that these 1-adamantylthiopyridines represent a novel class of antibacterial, antimalarial and anticancer agents with potential medicinal values.