| Autor: |
Suzuki, Takashi, Ikeda, Kiyoshi, Koyama, Noriko, Hosokawa, Chika, Kogure, Toshihiro, Takahashi, Tadanobu, Jwa Hidari, Kazuya, Miyamoto, Daisei, Tanaka, Kiyoshi, Suzuki, Yasuo |
| Zdroj: |
Glycoconjugate Journal; Apr2001, Vol. 18 Issue 4, p331-337, 7p |
| Abstrakt: |
Eleven novel analogs of 2-deoxy-2,3-didehydro- N-acetylneuraminic acid (Neu5Ac2en) modified at the C-4 and C-9 positions were designed and tested for their ability to inhibit sialidase of human parainfluenza virus type 1 (hPIV-1). The analogs modified by the cyanomethyl, amidinomethyl, and thiocarbamoylmethyl groups at the C-4 position exhibited potent inhibition against hPIV-1 sialidase compared with Neu5Ac2en. The most effective compound was thiocarbamoylmethyl analog (4- O-thiocarbamoylmethyl-Neu5Ac2en). The activity of 4- O-thiocarbamoylmethyl-Neu5Ac2en causing 50% enzyme inhibition at a concentration of approximately 1.0×10−5M was 30-fold larger than Neu5Ac2en. While, the analogs of Neu5Ac2en modified by the azido and N-acetyl groups at the C-9 showed a decrease in inhibition of sialidase compared with the 9-hydroxy analogs. In addition, 4- O-thiocarbamoylmethyl-Neu5Ac2en strongly inhibited hPIV-1 infections of Lewis lung carcinoma-monkey kidney cells in comparison with Neu5Ac2en. The present findings would provide useful information for the development of anti-human parainfluenza virus compounds. [ABSTRACT FROM AUTHOR] |
| Databáze: |
Complementary Index |
| Externí odkaz: |
|
Full text from SpringerLink