86207-79-6Relevant academic research and scientific papers
Synthesis and biological evaluation of prodrug-type anti-HIV agents: Ester conjugates of carboxylic acid-containing dipeptide HIV protease inhibitors and a reverse transcriptase inhibitor
Matsumoto, Hikaru,Matsuda, Takashi,Nakata, Shingo,Mitoguchi, Takatoshi,Kimura, Tooru,Hayashi, Yoshio,Kiso, Yoshiaki
, p. 417 - 430 (2001)
On the basis of substrate transition-state mimic concept of HIV protease, a series of small-sized dipeptide inhibitors containing hydrophilic carboxyl group were designed and synthesized. These dipeptide inhibitors showed good HIV protease inhibitory activity, but their anti-HIV activity was poor. The low antiviral activities of these inhibitors were probably due to their inadequate cell membrane permeability caused by the presence of a free carboxylic acid in the inhibitors. Based on the prodrug concept as well as the combination of two different classes of anti-HIV agents, conjugates of HIV protease inhibitors with a nucleoside reverse transcriptase inhibitor were synthesized. Some of these conjugates exhibited excellent antiviral activity compared with that of individual inhibitors. The synergistic enhancement of anti-HIV activities of these conjugates may be due to their ability to penetrate into the target cell and subsequent regeneration of two different classes of anti-HIV agents in the cytoplasm.
Antibacterial β-lactam compounds
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, (2008/06/13)
Novel β-lactam compounds classified into penem compounds, a process for preparing the same and use of such β-lactam compounds are disclosed. These β-lactam compounds exhibit excellent antimicrobial activities useful as pharmaceuticals or they are important intermediates for the synthesis of compounds having antimicrobial activities.
