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Titolo:
ACTIVITY AND STRUCTURE RELATIONSHIP OF ACRIDINE-DERIVATIVES AGAINST AFRICAN TRYPANOSOMES
Autore:
OBEXER W; SCHMID C; BARBE J; GALY JP; BRUN R;
Indirizzi:
SWISS TROP INST CH-4002 BASEL SWITZERLAND FAC PHARM MARSEILLE,GERCTOP,CNRS,URA 1411 F-13385 MARSEILLE FRANCE
Titolo Testata:
Tropical medicine and parasitology
fascicolo: 1, volume: 46, anno: 1995,
pagine: 49 - 53
SICI:
0177-2392(1995)46:1<49:AASROA>2.0.ZU;2-B
Fonte:
ISI
Lingua:
ENG
Soggetto:
INVITRO; AGENTS; DRUG;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
18
Recensione:
Indirizzi per estratti:
Citazione:
W. Obexer et al., "ACTIVITY AND STRUCTURE RELATIONSHIP OF ACRIDINE-DERIVATIVES AGAINST AFRICAN TRYPANOSOMES", Tropical medicine and parasitology, 46(1), 1995, pp. 49-53

Abstract

48 newly synthesized acridine derivatives of different classes were screened far antitrypanosomal activity. They showed a dose dependent effect on Trypanasoma rhodesiense and T. brucei bloodstream forms measured by the inhibition of esterase activity in a fluorescence based in vitro assay. After analysis of the IC50 and MIC values of the investigated acridines it was obvious that no new compound reached the level ofthe trypanocidal drugs in use (50 ng/ml). Most of the derivatives hadIC50 values in the range of 1 to 10 mu g/ml. 9 derivatives from different classes of acridines were in vitro active below 1 mu g/ml. Correlations between structure and effect on trypanosomes have been elucidated by comparing the IC50 and MIC values of these compounds, in the course of which no significant differences in the drug susceptibility between T. brucei und T. rhodesiense was noticed. The dialkylaminoalkyl derivatives among the group of the 9-thioacridines were slightly more potent than the mono-alkylated ones. 1,2,3,4-tetrahydro-9-thioacridinesshowed the influence of higher substituted side chains on the trypanocidal activity in the same way as 9-thioacridines, The corresponding ketones of 9-thioacridines confirmed the tendency of increasing toxicity due to the derivatisation of the dialkylaminoalkyl side chain. Within the series of the 9-aminoacridines the elongation of the side chain did not markedly change the activity, however the IC50 values are generally low between 0.13 and 1.2 mu g/ml. Two compounds belonging to monoalkylated-9-thioacridines showed to be 560 to 1000-fold less toxic for mammalian cells than for trypanosomes in vitro whereas the other compounds have been similarly active against human adenoma carcinoma cells and trypanosomes. Screening of the most active compounds in mice could not confirm the activity of these compounds expressed in vitro.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/01/21 alle ore 04:17:48