One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines
2011; Royal Society of Chemistry; Volume: 35; Issue: 11 Linguagem: Inglês
10.1039/c1nj20551j
ISSN1369-9261
AutoresGabin Mwande-Maguene, Jouda Jakhlal, Jean-Bernard Lékana-Douki, Elisabeth Mouray, Till Bousquet, Sylvain Pellegrini, Philippe Grellier, Fousseyni Samba Toure Ndouo, Jacques Lébibi, Lydie Pélinski,
Tópico(s)Synthesis and Biological Evaluation
ResumoAn efficient synthesis of 1,4-benzodiazepin-2-ones is described by condensation between 2-aminobenzophenone and Boc-protected amino acids via microwave-assisted irradiation. This produces higher yields in shorter reaction times than with traditional methods. The antiplasmodial activity of the corresponding ferrocenyl benzodiazepines was evaluated in vitro against Plasmodium falciparum F32 (chloroquine-sensitive) and FCB1 and K1 (chloroquine-resistant) strains and gabonese clinical isolates.
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