公开(公告)号：KR100738228B1

公开(公告)日：2007-07-12

申请号：KR1020060017423

申请日：2006-02-22

Applicant: 한국화학연구원

Inventor： 김범태 ,  민용기 ,  허정녕 ,  이혁 ,  이우길 ,  김성환 ,  박노균 ,  이윤정 ,  김형호

IPC: C07D401/06 ,  C07D417/06 ,  C07D413/06

Abstract: Antifungal azole compounds and a process for preparing the same compounds are provided to improve antifungal activity, especially against fluconazole-resistant Candida albicans, and minimize liver toxicity caused by long-term dosage by enhancing safety of the compounds against the human CytP450 enzyme. The antifungal triazole compounds represented by the formula(1), or pharmaceutically acceptable salts or isomers thereof are provided, wherein R is hydrogen or trifluoromethyl(CF3) group, and X is hydrogen or at least one halogen, C1-4 alkyl group, C1-4 haloalkyl group, C1-4 alkoxy group or dioxymethylene group. The antifungal triazole compounds represented by the formula(1) are prepared by reacting alcohol compounds represented by the formula(2) with styrene compounds represented by the formula(3) in the presence of base in organic solvent.

Abstract translation: 提供抗真菌唑化合物和制备相同化合物的方法以提高抗真菌活性，尤其是抗氟康唑耐药性白色念珠菌，并且通过增强化合物对人CytP450酶的安全性使长期剂量引起的肝毒性最小化。 提供了由式（1）表示的抗真菌三唑化合物或其药学上可接受的盐或异构体，其中R为氢或三氟甲基（CF 3），且X为氢或至少一个卤素，C 1-4烷基，C 1 -4卤代烷基，C1-4烷氧基或二氧化亚甲基。 由式（1）表示的抗真菌三唑化合物通过使式（2）表示的醇化合物与式（3）表示的苯乙烯化合物在碱存在下在有机溶剂中反应来制备。