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Pregled bibliografske jedinice broj: 369102

The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations

Džimbeg, Gabrijela; Rajić, Zrinka; Zorc, Branka; Kralj, Marijeta; Ester, Katja; Pavelić, Krešimir; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen
The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations // Abstracts of the 3rd Pharmaceutical Sciences World Congress
Amsterdam, Nizozemska, 2007. (poster, međunarodna recenzija, sažetak, znanstveni)

CROSBI ID: 369102 Za ispravke kontaktirajte CROSBI podršku putem web obrasca

Naslov
The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations

Autori
Džimbeg, Gabrijela ; Rajić, Zrinka ; Zorc, Branka ; Kralj, Marijeta ; Ester, Katja ; Pavelić, Krešimir ; Balzarini, Jan ; De Clercq, Erik ; Mintas, Mladen

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
Abstracts of the 3rd Pharmaceutical Sciences World Congress / - , 2007

Skup
Pharmaceutical Sciences World Congress (3 ; 2007)

Mjesto i datum
Amsterdam, Nizozemska, 22.04.2007. - 25.04.2007

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

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.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija



POVEZANOST RADA

Projekti:
098-0982464-2393 - Molekularna obilježja miofibroblasta Dupuytrenove bolesti
098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Kralj, Marijeta, MZOS ) ( CroRIS)
006-0000000-3216 - Sinteza, karakterizacija i djelovanje potencijalnih i poznatih ljekovitih tvari (Zorc, Branka, MZOS ) ( CroRIS)
125-0982464-2922 - RAZVOJ NOVIH PROLIJEKOVA I LIJEKOVA PROTIV VIRUSA I RAKA (Mintas, Mladen, MZOS ) ( CroRIS)

Ustanove:
Farmaceutsko-biokemijski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

Profili:

Avatar Url Zrinka Rajić (autor)

Avatar Url Krešimir Pavelić (autor)

Avatar Url Branka Zorc (autor)

Avatar Url Mladen Mintas (autor)

Avatar Url Marijeta Kralj (autor)

Avatar Url Katja Ester (autor)

Citiraj ovu publikaciju:

Džimbeg, Gabrijela; Rajić, Zrinka; Zorc, Branka; Kralj, Marijeta; Ester, Katja; Pavelić, Krešimir; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen
The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations // Abstracts of the 3rd Pharmaceutical Sciences World Congress
Amsterdam, Nizozemska, 2007. (poster, međunarodna recenzija, sažetak, znanstveni)
Džimbeg, G., Rajić, Z., Zorc, B., Kralj, M., Ester, K., Pavelić, K., Balzarini, J., De Clercq, E. & Mintas, M. (2007) The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations. U: Abstracts of the 3rd Pharmaceutical Sciences World Congress.
@article{article, author = {D\v{z}imbeg, Gabrijela and Raji\'{c}, Zrinka and Zorc, Branka and Kralj, Marijeta and Ester, Katja and Paveli\'{c}, Kre\v{s}imir and Balzarini, Jan and De Clercq, Erik and Mintas, Mladen}, year = {2007}, keywords = {primaquine, malaria, urea, cytostatic activity}, title = {The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations}, keyword = {primaquine, malaria, urea, cytostatic activity}, publisherplace = {Amsterdam, Nizozemska} }
@article{article, author = {D\v{z}imbeg, Gabrijela and Raji\'{c}, Zrinka and Zorc, Branka and Kralj, Marijeta and Ester, Katja and Paveli\'{c}, Kre\v{s}imir and Balzarini, Jan and De Clercq, Erik and Mintas, Mladen}, year = {2007}, keywords = {primaquine, malaria, urea, cytostatic activity}, title = {The novel primaquine derivatives of N-alkyl, cycloalkyl or aryl urea: synthesis, cytostatic and antiviral activity evaluations}, keyword = {primaquine, malaria, urea, cytostatic activity}, publisherplace = {Amsterdam, Nizozemska} }

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