• Archives of Pharmacal Research
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• v.17 no.6
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• pp.483-486
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• 1994

A series of 6-[N-(halophenyl)amino]-7-chloro-5, 8-quinolinedione derivatives 1-10 were tested for antifungal susceptibilities, in vitro, aginst pathogenic Candida species such as C. ablbicans, C glabrata, C. krusei, C. parapsilosis and C. tropicalis. The MICs were determined by the standard macrodilution techniques, according to the NCCLS 1992 guidelines. The 6-[N-(halo-standard macrodilution techniques, according to the NCCLS 1992 gidelines. The 6-[N-(halo-phenyl)amino]-7-chloro-5, 8-quinolinedione derivatives showed generally potent antifungal activities against pathogenic Candida species. Among them, derivative 1, 2, 5, and 7 showed more potent antifungal activities than kietoconazole. All derivatives 1-10 had specially potent activities against C. torpicalis. Derivative 1 and 2 containing 9N-3, 4-dihalo-phenyl)amino moiety exhibited the potent antifugal activities. Derivative 2 with (3, 4-dichlorophenyl)amino substitutent was the most effetive in preventing the growth of Candida species at MICs 4.mu.g/ml respectively.

• Journal of Food Hygiene and Safety
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• v.14 no.3
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• pp.282-286
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• 1999

OQ-21을 암·수 ICR계 마우스에 복강투여 하여 급성독성을 측정한 결과 최대용량 투여군에서도 사망한 동물은 관찰되지 않았다. 그리고 시험동물을 부검하여 육안 관찰한 결과 OQ-21 투여군은 대조군과 전혀 차이가 없었고 실제 독성도 비교적 낮은 것으로 판단된다. 또한 OQ-21이 혈과에 수축 반응에 영향을 미치는 지를 연구한 결과 용량 의존적으로 phenylephirne에 의한 혈관 수축을 증가시킴을 관찰하였다. 이상의 결과로부터 OQ-21은 급성독성이 약한 것으로 생각되지만 혈관 수축에 미치는 영향은 앞으로 인체 안전성에 관하여 검토하여야 할 과제로 사료된다.

• Bulletin of the Korean Chemical Society
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• v.23 no.3
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• pp.417-422
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• 2002

Comparison studies of the Quantitative Structure Activity Relationship (QSAR) methods with new imidazo-quinolinedione derivatives were conducted using Comparative Molecular Field Analysis (CoMFA), Comparative Molecular Similarity Indices Analysis (CoMSIA), and the Hologram Quantitative Structure Activity Relationship (HQSAR). When the CoMFA crossvalidation value, q2, was 0.625, the Pearson correlation coefficient, r2, was 0.973. In CoMSIA, q2 was 0.52 and r2 was 0.979. In the HQSAR, q2 was 0.501 and r2 was 0.924. The best result was obtained using the CoMSIA method according to a comparison of the calculated values with the real in vitro cytotoxic activities against human ovarian cancer cell lines.