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Titolo:
Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs
Autore:
Klenke, B; Stewart, M; Barrett, MP; Brun, R; Gilbert, IH;
Indirizzi:
Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3XF, S Glam, Wales Cardiff Univ Cardiff S Glam Wales CF10 3XF ardiff CF10 3XF, S Glam, Wales Univ Glasgow, Inst Biomed & Life Sci, Div Infect & Immun, Glasgow G12 8QQ,Lanark, Scotland Univ Glasgow Glasgow Lanark Scotland G12 8QQ gow G12 8QQ,Lanark, Scotland Swiss Trop Inst, CH-4002 Basel, Switzerland Swiss Trop Inst Basel Switzerland CH-4002 st, CH-4002 Basel, Switzerland
Titolo Testata:
JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 21, volume: 44, anno: 2001,
pagine: 3440 - 3452
SICI:
0022-2623(20011011)44:21<3440:SABEOS>2.0.ZU;2-I
Fonte:
ISI
Lingua:
ENG
Soggetto:
HUMAN AFRICAN TRYPANOSOMIASIS; CRUZI TRYPANOTHIONE REDUCTASE; UNUSUAL ADENOSINE TRANSPORTER; IN-VITRO; ANTITRYPANOSOMAL ACTIVITY; BRUCEI-BRUCEI; DERIVATIVES; MELARSOPROL; INHIBITORS; ANALOGS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
47
Recensione:
Indirizzi per estratti:
Indirizzo: Gilbert, IH Cardiff Univ, Welsh Sch Pharm, Redwood Bldg,King Edward VII Ave, Cardiff CF10 3XF, S Glam, Wales Cardiff Univ Redwood Bldg,King Edward VII Ave Cardiff S Glam Wales CF10 3XF
Citazione:
B. Klenke et al., "Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs", J MED CHEM, 44(21), 2001, pp. 3440-3452

Abstract

The P2 transporter is a nucleoside transporter which is unique to the protozoan parasite Trypanosoma brucei, the causative organism of Human African Trypanosomasis. The transporter has been shown to bind some structural motifs not recognized by other transporters. In this paper we describe the use of the melamine motif, a substrate of the P2 transporter, as a potential tool to selectively deliver polyamine analogues to the parasites. The synthesis of a number of polyamine analogues attached to a variety of melamine analogues is described. Many of the compounds were shown to competitively inhibit uptake of adenosine, indicating that they are recognized by the transporter. Some of the compounds showed good in vitro activity against the parasites.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/01/21 alle ore 04:06:50