Synthesis and antimalarial activity of novel hydroxyethylamines, potential aspartyl protease inhibitors

被引：13
作者：
Cunico, Wilson [1 ]
G. Ferreira, Maria de Lourdes [1 ]
Ferreira, Thais G. [1 ]
Penido, Carmen [2 ]
M. O. Henriques, Maria G. [2 ]
Krettli, Luisa G. [3 ,4 ]
Varotti, Fernando P. [3 ,4 ]
Krettli, Antoniana U. [3 ,4 ]
机构：
[1] Fiocruz MS, Inst Tecnol Farmacos Farmanguinhos, BR-21041250 Rio De Janeiro, Brazil
[2] Inst Tecnol Farmacos Farmanguinhos, Dept Farmacol Aplicada, Rio De Janeiro, Brazil
[3] Univ Fed Minas Gerais, Fiocruz, Ctr Pesquisas Rene Rachou, Belo Horizonte, MG, Brazil
[4] Univ Fed Minas Gerais, Dept Parasitol, Belo Horizonte, MG, Brazil
来源：
LETTERS IN DRUG DESIGN & DISCOVERY | 2008年 / 5卷 / 03期
关键词：
hydroxyethylamine; antimalarial; protease inhibitors;
D O I：
10.2174/157018008784083938
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Parasite resistance to antimalarial drugs is a serious threat to human health, and novel agents that act on essential enzymes for parasite metabolism, such as proteases, are attractive targets for drug development. In this work, the antimalarial activity of hydroxyethylamine derivatives have been evaluated in vitro against Plasmodium falciparum W2 clone chloroquine resistant. These results show that the some compounds have moderated activity against malaria parasite.
引用
收藏
页码：178 / 181
页数：4
相关论文
共 20 条
[1]   Potencies of human immunodeficiency virus protease inhibitors in vitro against Plasmodium falciparum and in vivo against murine malaria [J].
Andrews, KT ;
Fairlie, DP ;
Madala, PK ;
Ray, J ;
Wyatt, DM ;
Hilton, PM ;
Melville, LA ;
Beattie, L ;
Gardiner, DL ;
Reid, RC ;
Stoermer, MJ ;
Skinner-Adams, T ;
Berry, C ;
McCarthy, JS .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2006, 50 (02) :639-648
[2]   LARGE-SCALE PREPARATION OF (2S,3S)-N-BOC-3-AMINO-1,2-EPOXY-4-PHENYLBUTANE - A KEY BUILDING-BLOCK FOR HIV-PROTEASE INHIBITORS [J].
BEAULIEU, PL ;
WERNIC, D ;
DUCEPPE, JS ;
GUINDON, Y .
TETRAHEDRON LETTERS, 1995, 36 (19) :3317-3320
[3]   Inhibitors of the Plasmodium falciparum parasite aspartic protease plasmepsin II as potential antimalarial agents [J].
Boss, C ;
Richard-Bildstein, S ;
Weller, T ;
Fischli, W ;
Meyer, S ;
Binkert, C .
CURRENT MEDICINAL CHEMISTRY, 2003, 10 (11) :883-907
[4]   Aspartic proteases of Plasmodium falciparum and other parasitic protozoa as drug targets [J].
Coombs, GH ;
Goldberg, DE ;
Klemba, M ;
Berry, C ;
Kay, J ;
Mottram, JC .
TRENDS IN PARASITOLOGY, 2001, 17 (11) :532-537
[5]   Antimalarial activity of 4-(5-trifluoromethyl-1H-pyrazol-1-yl)chloroquine analogues [J].
Cunico, W ;
Cechinel, CA ;
Bonacorso, HG ;
Martins, MAP ;
Zanatta, N ;
de Souza, MVN ;
Freitas, IO ;
Soares, RPP ;
Krettli, AU .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (03) :649-653
[6]   Aspartic peptidase inhibitors: Implications in drug development [J].
Dash, C ;
Kulkarni, A ;
Dunn, B ;
Rao, M .
CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY, 2003, 38 (02) :89-119
[7]   Antimalarial activity of phenazines from lapachol, β-lapachone and its derivatives against Plasmodium falciparum in vitro and Plasmodium berghei in vivo [J].
de Andrade-Neto, VF ;
Goulart, MOF ;
da Silva, JF ;
da Silva, MJ ;
Pinto, MD ;
Pinto, AV ;
Zalis, MG ;
Carvalho, LH ;
Krettli, AU .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2004, 14 (05) :1145-1149
[8]   QUANTITATIVE ASSESSMENT OF ANTI-MALARIAL ACTIVITY INVITRO BY A SEMIAUTOMATED MICRODILUTION TECHNIQUE [J].
DESJARDINS, RE ;
CANFIELD, CJ ;
HAYNES, JD ;
CHULAY, JD .
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 1979, 16 (06) :710-718
[9]   Macrocyclic inhibitors of the malarial aspartic proteases plasmepsin I, II, and IV [J].
Ersmark, K ;
Nervall, M ;
Gutiérrez-de-Terán, H ;
Hamelink, E ;
Janka, LK ;
Clemente, JC ;
Dunn, BM ;
Gogoll, A ;
Samuelsson, B ;
Åqvist, J ;
Hallberg, A .
BIOORGANIC & MEDICINAL CHEMISTRY, 2006, 14 (07) :2197-2208
[10]   MTT COLORIMETRIC ASSAY FOR TESTING MACROPHAGE CYTOTOXIC ACTIVITY INVITRO [J].
FERRARI, M ;
FORNASIERO, MC ;
ISETTA, AM .
JOURNAL OF IMMUNOLOGICAL METHODS, 1990, 131 (02) :165-172
12