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Titolo:
(S)-9-(3-HYDROXY-2-PHOSPHONYLMETHOXYPROPYL)ADENINE [(S)-HPMPA] - A PURINE ANALOG WITH TRYPANOCIDAL ACTIVITY IN-VITRO AND IN-VIVO
Autore:
KAMINSKY R; SCHMID C; GRETHER Y; HOLY A; DECLERCQ E; NAESENS L; BRUN R;
Indirizzi:
SWISS TROP INST,SOCINSTR 57 CH-4002 BASEL SWITZERLAND ACAD SCI CZECH REPUBL,INST ORGAN CHEM & BIOCHEM PRAGUE CZECH REPUBLIC KATHOLIEKE UNIV LEUVEN,REGA INST MED RES LOUVAIN BELGIUM
Titolo Testata:
TM & IH. Tropical medicine & international health
fascicolo: 2, volume: 1, anno: 1996,
pagine: 255 - 263
SICI:
1360-2276(1996)1:2<255:([-AP>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
DL-ALPHA-DIFLUOROMETHYLORNITHINE; TRYPANOSOMA-BRUCEI-RHODESIENSE; BLOOD-STREAM FORMS; DNA VIRUS AGENT; SLEEPING SICKNESS; DRUG-RESISTANCE; INVITRO; DERIVATIVES; CONGOLENSE; GAMBIENSE;
Keywords:
AFRICAN TRYPANOSOMES; CHEMOTHERAPY; PURINES; (S)-HPMPA; IN VITRO ASSAYS; CYTOTOXICITY;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
37
Recensione:
Indirizzi per estratti:
Citazione:
R. Kaminsky et al., "(S)-9-(3-HYDROXY-2-PHOSPHONYLMETHOXYPROPYL)ADENINE [(S)-HPMPA] - A PURINE ANALOG WITH TRYPANOCIDAL ACTIVITY IN-VITRO AND IN-VIVO", TM & IH. Tropical medicine & international health, 1(2), 1996, pp. 255-263

Abstract

The unique features of purine salvage systems of pathogenic haemoflagellates render them selectively susceptible to the cytotoxic effects of purine analogues. A series of acyclic nucleoside phosphonates were evaluated for activity against pathogenic haemoflagellates in vitro. One of the phosphonylmethoxyalkylpurines, namely (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine [(S)-HPMPA], was active in vitro against bloodstream forms of Trypanosoma brucei rhodesiense, T. b. gambiense, multidrug-resistant T. b. brucei, T. congolense and T. evansi, but not against intracellular T. cruzi or Leishmania donovani. Cytotoxic effects against mammalian cells were observed at 4900-27 300-fold higher concentrations than those necessary to inhibit T. b. rhodesiense. (S)-HPMPA was able to eliminate T. b. rhodesiense and multidrug-resistant T.b. brucei in an acute rodent model with two administrations of 10 mg/kg each.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 18/01/21 alle ore 14:29:05