One-pot microwave-assisted synthesis and antimalarial activity of ferrocenyl benzodiazepines

被引：16

作者：

Mwande-Maguene, Gabin ^{[2
]}

Jakhlal, Jouda ^{[2
]}

Lekana-Douki, Jean-Bernard ^{[3
]}

Mouray, Elisabeth ^{[4
]}

Bousquet, Till ^{[2
]}

Pellegrini, Sylvain ^{[2
]}

Grellier, Philippe ^{[4
]}

Ndouo, Fousseyni Samba Toure ^{[3
]}

Lebibi, Jacques ^{[1
]}

Pelinski, Lydie ^{[2
]}

机构：

[1] Univ Sci & Tech Masuku, Franceville, Gabon

[2] Univ Lille 1, ENSCL, CNRS,UMR 8181, Univ Lille Nord France,Unite Catalyse & Chim Soli, F-59652 Villeneuve Dascq, France

[3] CIRMF, Unite Parasitol, Franceville, Gabon

[4] Museum Natl Hist Nat, CNRS, MCAM, Dept Regulat Dev Diversite Mol,FRE 3206, F-75231 Paris, France

来源：

NEW JOURNAL OF CHEMISTRY | 2011年 / 35卷 / 11期

关键词：

IN-VITRO; PLASMODIUM-FALCIPARUM; COMBINATORIAL SYNTHESIS; TOXOPLASMA-GONDII; INHIBITORS; DERIVATIVES; RECEPTOR; FERROQUINE; CHILDREN; SEIZURES;

D O I：

10.1039/c1nj20551j

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An 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.

引用

页码：2412 / 2415

页数：4

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