Abstract:
:The synthesis of four new computer-designed fluoroquinolones which have been predicted by QSAR analysis to be active against the protozoa Toxoplasma gondii is described. These compounds are inhibitory in vitro for T. gondii. One of these compounds has a remarkably high activity comparable to that of trovafloxacin. It combines the basic cyclopropyl-quinoline structure of gatifloxacin or moxifloxacin with the C-7 6-amino-3-azabicyclo[3.1.0]hexyl side chain of trovafloxacin. The four compounds are also inhibitory for blood stages of Plasmodium falciparum though at high concentration. These results confirm the potential of quinolones as anti-T. gondii and antimalarial drugs but also show that the QSAR models for T. gondii cannot be reliably extended for screening antimalarial activity.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Anquetin G,Rouquayrol M,Mahmoudi N,Santillana-Hayat M,Gozalbes R,Greiner J,Farhati K,Derouin F,Guedj R,Vierling Pdoi
10.1016/j.bmcl.2004.03.070subject
Has Abstractpub_date
2004-06-07 00:00:00pages
2773-6issue
11eissn
0960-894Xissn
1464-3405pii
S0960894X04004421journal_volume
14pub_type
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