Chand Pooran, Bantia Shanta, Kotian Pravin L, El-Kattan Yahya, Lin Tsu-Hsing, Babu Yarlagadda S
BioCryst Pharmaceuticals, Inc., 2190 Parkway Lake Drive, Birmingham, AL 35244, USA.
Bioorg Med Chem. 2005 Jun 2;13(12):4071-7. doi: 10.1016/j.bmc.2005.03.048. Epub 2005 Apr 25.
Cyclopentane derivatives, designated as BCX-1812, BCX-1827, BCX-1898, and BCX-1923, were tested in parallel with oseltamivir carboxylate and zanamivir for the in vivo activity in mice infected with A/Turkey/Mas/76 X A/Beijing/32/92 (H6N2) influenza virus. The compounds were tested orally and intranasally at different dose levels. BCX-1812, BCX-1827, and BCX-1923 showed more than 50% protection at 1mg/kg/day dose level on oral treatment. The intranasal treatment was 100% effective even at 0.01 mg/kg/day for all four compounds. On comparison with oseltamivir carboxylate and zanamivir, these four cyclopentane derivatives have shown equal or better efficacies. The synthesis of two new compounds, BCX-1898 and BCX-1923, is also described.
将名为BCX - 1812、BCX - 1827、BCX - 1898和BCX - 1923的环戊烷衍生物与奥司他韦羧酸盐和扎那米韦同时进行测试，以研究其对感染A/土耳其/马斯/76 X A/北京/32/92（H6N2）流感病毒的小鼠的体内活性。这些化合物在不同剂量水平下进行口服和鼻内给药测试。口服治疗时，BCX - 1812、BCX - 1827和BCX - 1923在1mg/kg/天的剂量水平下显示出超过50%的保护率。对于所有四种化合物，鼻内治疗即使在0.01mg/kg/天的剂量下也有100%的疗效。与奥司他韦羧酸盐和扎那米韦相比，这四种环戊烷衍生物显示出相同或更好的疗效。文中还描述了两种新化合物BCX - 1898和BCX - 1923的合成方法。
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