Inhibitory effects of triterpene-azidothymidine conjugates on proliferation of human immunodeficiency virus type 1 and its protease.
The conjugates of some dicarboxylic acid hemiesters of triterpenes which show potent inhibition against human immunodeficiency virus type 1 protease (HIV-1 PR) with a reverse transcriptase inhibitor azidothymidine (AZT) or anti-HIV alkaloid FK 3000 were prepared, and their inhibitory activities were investigated against HIV-induced cytopathic effects (CPE) and HIV-1 PR. Most of the triterpene-AZT conjugates showed potent anti-HIV activity as well as moderate to potent PR inhibitory activity, though AZT itself showed no PR inhibitory activity at all. However, the triterpene-FK 3000 conjugates showed neither PR inhibitory activity nor anti-HIV activity.
Ma
Chao-Mei
CM
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Sugitani, Japan.
Nakamura
Norio
N
Hattori
Masao
M
Kawahata
Takuya
T
Otake
Toru
T
D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D017320:HIV Protease Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects* / Q000201:enzymology; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D015215:Zidovudine / Q000737:chemistry / Q000494:pharmacology*
D019380:Anti-HIV Agents; D017320:HIV Protease Inhibitors; D018894:Reverse Transcriptase Inhibitors; D014315:Triterpenes; D015215:Zidovudine