Abstract:
:Derivatives of 7-benzylidenenaltrexone (BNTX), which was recently reported to be an effective chloroquine (CQ)-resistance reverser, were synthesized and evaluated for their CQ-resistance reversing activities. The synthesized derivatives showed CQ-resistance reversing effects. They also reacted with glutathione (GSH) both enzymatically and chemically, and inhibited glutathione reductase activity. 7-Benzyl derivative, which was obtained by reduction of the olefin group in α,β-unsaturated ketone structure of BNTX, also exhibited CQ-resistance reversing effect, but its potency was significantly lower than that of BNTX. These outcomes suggested that the decrease in GSH level could be one of the mechanisms of CQ-resistance reversing effects induced by BNTX derivatives.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Miyata Y,Fujii H,Uenohara Y,Kobayashi S,Takeuchi T,Nagase Hdoi
10.1016/j.bmcl.2012.06.085subject
Has Abstractpub_date
2012-08-15 00:00:00pages
5174-6issue
16eissn
0960-894Xissn
1464-3405pii
S0960-894X(12)00845-1journal_volume
22pub_type
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