Effect of quinolinedione derivative (OQ-21) on phenylephrine induced vasoconstriction was investigated using aortic rings in organ bath isolated from rats. Treatment with OQ-21 resulted in moderate increase in vasoconstriction in a dose-dependent manner. In addition we studied acute intraperitoneal toxicity of OQ-21 in male and female ICR mice. The changes of body weight and clinical signs were observed for 7 days after single dose of OQ-21 from 50 mg/kg to 500 mg/kg. There were no significant changes in body weight and clinical signs. Any mouse didn't die even at maximal dose. Autopsy of OQ-21 treated mice revealed no abnormal difference from contol mice, These results suggest that OQ-21 be moderately safe and could be developed as effective drug.

6-(4-Iodophenyl)amino-7-chloro-5,8-quinolinedione (RCK9) was evaluated for antifungal activities. The MIC values of RCK9 were determined against A. flavus, C. albicans, C. neoformans and F. oxysporium. The RCK9 showed generally potent antifungal activities against the tested fungi. Acute oral toxicity studies of RCK9 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK9 were low and LDSO values were over 2,850 mg/kg in ICR mice. The genotoxicities of RCK9 had been evaluated. RCK9 was negative in Ames test with Salmonella typhimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK9 with in vivo mouse micronucleus assay. RCK9 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. The results indicate that RCK9 has no genotoxic potential under these experimental conditions.

6-[(N-3,4-Dibromophenyl)amino]-7-chloro-5,8-quinolinedione(RCK13) was tested for antifungal activities. The MIC values were determined by the two-fold dilution method. The therapeutic potential of RCK13 had been assessed in comparison with ketoconazole and fluconazole against systemic infections with Candida albicans in normal mice. RCK13 had ED_(50), 0.80±0.21 mg/kg but ketoconazole had ED_(50), 8.00±0.73 mg/kg respectively. And administered RCK13 at the ED_(50) for 14 days improved survival rates as well as ketoconazole. Acute oral toaicity studies of RCK13 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK13 were low and LD_(50) values were over 2,850 mg/kg in ICR mice. The genotoxicities of RCK 13 had been evaluated. RCK13 was negative in Ames test with Salmonella ryphimurium and chromosomal aberration test in CHL cells. The clastogenicity was tested on the RCK13 with in vivo mouse micronucleus assay. RCK13 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK13 has no genotoxic potential under these experimental conditions.

Eight natural or semisynthesized monoterpenes were examined for their effects on rat brain monoamine oxidase(MAO) using benzylamine as substrate. Thujone and 3-carene were found to have the inhibition effects on rat brain MAO activity; 38% and 95% inhibition at 10^(-3) M respectively. The kinetic study on 3-carene, the most potent inhibitor tested in this study, showed that its MAO inhibition effect was confirmed as uncompetetive type. But (+) pulegon and (-) isopulegon was found to activate MAO slightly.