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Pregled bibliografske jedinice broj: 369102

Zbornik radova

Autori: Džimbeg, Gabrijela; Rajić, Zrinka; Zorc, Branka; Kralj, Marijeta; Ester, Katja; Pavelić, Krešimir; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen
Naslov: The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations
Izvornik: Abstracts of the 3rd Pharmaceutical Sciences World Congress
Skup: Pharmaceutical Sciences World Congress (3 ; 2007)
Mjesto i datum: Amsterdam, Nizozemska, 22-25.04.2007.
Ključne riječi: primaquine; malaria; urea; cytostatic activity
Sažetak:
Primaquine, N4-(6-methoxy-8-quinolinyl)-1, 4-pentanediamine, is known antimalarial drug that is active against both the latent liver forms of the relapsing malaria caused by Plasmodium vivax and Plasmodium ovale and the gametocytes from all species of parasite causing human malaria, including chloroquine-resistant Plasmodium falciparum. The novel urea primaquine derivatives 3a-i were prepared by aminolysis of benzotriazolide 2 with the corresponding amine in the presence or absence of triethylamine. In order to obtain the targeted derivatives of urea 3a-i with different lipophilicity, various aliphatic and aromatic primary or secondary amines were used for their synthesis (diethylamine, cyclopentylamine, cyclohexylamine, cyclohexanemethylamine, dicyclohexylamine, 2-phenylethylamine, 4-(aminomethyl)pyridine and benzhydrylamine). Compound 2 was prepared by acylation of primaquine with 1-benzotriazole carboxylic acid chloride. Among all compounds evaluated, the pyridine derivative 3h exhibited the best cytostatic activities against colon carcinoma, human T-lymphocyte and murine leukemia. However, this compound showed also rather marked cytotoxicity towards human normal fibroblasts. The highest selectivity in the inhibitory effects on human malignant tumour cell lines vs. normal fibroblasts was found for ureas 3c, 3d and 3g. Results of broad antiviral evaluation showed that pyridine and phenethyl derivatives of urea 3h and 3g exhibited some selective inhibition against cytomegalovirus.
Vrsta sudjelovanja: Poster
Vrsta prezentacije u zborniku: Sažetak
Vrsta recenzije: Međunarodna recenzija
Projekt / tema: 006-0000000-3216, 098-0982464-2514, 098-0982464-2393, 125-0982464-2922
Izvorni jezik: ENG
Kategorija: Znanstveni
Znanstvena područja:
Kemija,Temeljne medicinske znanosti,Farmacija
Upisao u CROSBI: bzorc@pharma.hr (bzorc@pharma.hr), 23. Lis. 2008. u 10:57 sati



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