Abstract：
:Naltrexone (1), which is a member of the group of competitive opioid antagonists, shows a strong affinity for mu-receptors and its derivatives have been notable as novel receptor antagonists. In this paper, the preparation of several naltrexone derivatives is described; these were used to investigate the role of the oxygenated functional groups in facilitating binding to a series of the opioid receptors. The derivatives showed affinity for opioid mu-receptors which was similar to that of naltrexone, but these compounds, which had masked hydroxyl functional groups, displayed a moderate activity. These results suggest that every oxygenated functional group in naltrexone (1) plays an important role in binding to the opioid receptor.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Uwai K,Uchiyama H,Sakurada S,Kabuto C,Takeshita Mdoi
10.1016/j.bmc.2003.10.039subject
Has Abstractpub_date
2004-01-15 00:00:00pages
417-21issue
2eissn
0968-0896issn
1464-3391pii
S0968089603007247journal_volume
12pub_type
杂志文章abstract：:The synthesis and structure-activity relationships of a series of simple biphenyls is described. Optimization of the 4-hydroxy-biphenyl template led to compounds with ERbeta selectivity on the order of 20-70-fold. ...
journal_title：Bioorganic & medicinal chemistry
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abstract：:The emergence of multidrug-resistant bacterial and fungal strains poses a threat to human health that requires the design and synthesis of new classes of antimicrobial agents. We evaluated bis(N-amidinohydrazones) and N-(amidino)-N'-aryl-bishydrazones for their antibacterial and antifungal activities against panels of...
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journal_title：Bioorganic & medicinal chemistry
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journal_title：Bioorganic & medicinal chemistry
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