Ohkubo M, Kuno A, Sakai H, Sugiyama Y, Takasugi H
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Chem Pharm Bull (Tokyo). 1994 Jun;42(6):1279-85. doi: 10.1248/cpb.42.1279.
Novel pyrimidine derivatives, possessing linkages between the aryl group and the pyrimidine nucleus at the C-4 position, were prepared and tested for anti-anoxic (AA) activity in mice. Among them, 5-(4-methylpiperazin-1-ylcarbonyl)-4-(4-nitrobenzoyl)-2-p henylpyrimidine (2f, FR76659) possessed significant AA activity (10-100 mg/kg, i.p.) with low acute toxicity (LD50 > 1000 mg/kg, i.p.). Structure-activity relationships in regard to AA activity of this series of compounds were examined.
制备了在芳基与嘧啶核的C-4位之间具有连接键的新型嘧啶衍生物，并在小鼠中测试了其抗缺氧（AA）活性。其中，5-(4-甲基哌嗪-1-基羰基)-4-(4-硝基苯甲酰基)-2-苯基嘧啶（2f，FR76659）具有显著的AA活性（腹腔注射，10-100mg/kg），且急性毒性较低（腹腔注射，LD50>1000mg/kg）。研究了该系列化合物AA活性的构效关系。
