Catalogo Articoli (Spogli Riviste)

OPAC HELP

Titolo:
IN-VITRO TRYPANOCIDAL ACTIVITIES OF NEW S-ADENOSYLMETHIONINE DECARBOXYLASE INHIBITORS
Autore:
BRUN R; BUHLER Y; SANDMEIER U; KAMINSKY R; BACCHI CJ; RATTENDI D; LANE S; CROFT SL; SNOWDON D; YARDLEY V; CARAVATTI G; FREI J; STANEK J; METT H;
Indirizzi:
SWISS TROP INST CH-4002 BASEL SWITZERLAND CIBA GEIGY LTD,DIV PHARMACEUT CH-4002 BASEL SWITZERLAND PACE UNIV,HASKINS LABS NEW YORK NY 10038 PACE UNIV,DEPT BIOL NEW YORK NY 10038 UNIV LONDON LONDON SCH HYG & TROP MED,DEPT MED PARASITOL LONDON WC1E 7HT ENGLAND
Titolo Testata:
Antimicrobial agents and chemotherapy
fascicolo: 6, volume: 40, anno: 1996,
pagine: 1442 - 1447
SICI:
0066-4804(1996)40:6<1442:ITAONS>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
TRYPANOSOMA-BRUCEI-BRUCEI; DL-ALPHA-DIFLUOROMETHYLORNITHINE; METHYLGLYOXAL BIS(GUANYLHYDRAZONE); RHODESIENSE; INVITRO; METHYLGLYOXAL-BIS(GUANYLHYDRAZONE); CULTIVATION; RESISTANCE; POLYAMINES; ANALOGS;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
R. Brun et al., "IN-VITRO TRYPANOCIDAL ACTIVITIES OF NEW S-ADENOSYLMETHIONINE DECARBOXYLASE INHIBITORS", Antimicrobial agents and chemotherapy, 40(6), 1996, pp. 1442-1447

Abstract

A series of novel aromatic derivatives based on the structure of methylglyoxal bis(guanylhydrazone) (MGBG) was examined for in vitro antitrypanosomal activities and cytotoxicities for human cells, One-third ofthe compounds tested showed trypanocidal activity at concentrations below 0.5 mu M after an Incubation period of 72 h, Structure-activity analysis revealed that bicyclic compounds with homocyclic rings and unmodified termini were the most active compounds, Results obtained in three laboratories employing different methods and trypanosome populations consistently ranked compound CGP 40215A highest, This compound had a 50% inhibitory concentration of 0.0045 mu M for Trypanosoma brucei rhodesiense, was also active against other trypanosome species, including a multidrug-resistant Trypanosoma brucei brucei, and was significantly less toxic than other compounds tested for a human adenocarcinoma cell line, with a 50% inhibitory concentration of 1.14 mM. The effect of CGP 40215A was time and dose dependent, and low concentrations of the compound required exposure times of > 2 days to exert trypanocidal activity, Compounds were inactive against Leishmania donovani and Trypanosoma cruzi amastigotes in murine macrophages in vitro.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 23/01/21 alle ore 02:50:54