Comparison of the anti-influenza virus activity of cyclopentane derivatives with oseltamivir and zanamivir in vivo |
| |
Authors: | Chand Pooran Bantia Shanta Kotian Pravin L El-Kattan Yahya Lin Tsu-Hsing Babu Yarlagadda S |
| |
Affiliation: | BioCryst Pharmaceuticals, Inc., 2190 Parkway Lake Drive, Birmingham, AL 35244, USA. pchand@biocryst.com |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|