Abstract：
:Several strychnobrasiline derivatives have been synthesized to overcome the lack of in vivo reversal activity of the parent compound. In the present study, N(a)-deacetyl-ferrocenoyl-strychnobrasiline was synthesized by condensing N(a)-deacetyl-strychnobrasiline with ferrocenic acid previously treated with oxalyl chloride. While the in vitro antiplasmodial activity of the test compound (IC(50)=4.83 microg/mL) was increased 15-fold compared to that of strychnobrasiline, and the in vitro enhancing activity was found to be similar to that of the parent compound, the compound was devoid of any in vivo potentiating effect, and an antagonistic effect was even observed at higher doses. Based on the overall results on the hemisynthesis of strychnobrasiline derivatives for better reversal activity, this strategy has appeared to be of little value for useful drugs.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Razafimahefa D,Pélinski L,Martin MT,Ramanitrahasimbola D,Rasoanaivo P,Brocard Jdoi
10.1016/j.bmcl.2004.11.067subject
Has Abstractpub_date
2005-02-15 00:00:00pages
1239-41issue
4eissn
0960-894Xissn
1464-3405pii
S0960-894X(04)01438-6journal_volume
15pub_type
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