Saber UCV
Repositorio Institucional
Repositorio Institucional
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https://saber.ucv.ve/handle/10872/3868
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| Title: | Arch Venez Med Trop |
| Authors: | León, Caritza Domínguez, José Rojas, Danelis Rodrigues, Juan Gamboa, Neira Gut, Jiri Rosenthal, Phillip |
| Issue Date: | 2007 |
| Publisher: | Rev Invest |
| Abstract: | We described the synthesis of 3-chloro-2N-[1 -alkyl-1 -(4 - chlorophenylcarbamoyl) methyl]amine-1,4-naphthoquinones derivatives. The new compounds were characterized through IR, 1H NMR, 13C NMR and Mass Spectrometry. The biological evaluation of these derivatives was carry out by inhibition of beta-hematin formation in vitro and the inhibition of cultured P. falciparum parasites. The most active compound resulted the 3-chloro-2N-[1 -methyl-1 -(4 -chlorophenylcarbamoyl) methyl] amine-1,4-naphthoquinone 15, Cl50 1.92 μM, as an inhibitor in cultured P. falciparum parasites, while compound 3-chloro-2N-[1 -(phenylmethyl)- 1 -(4 -chlorophenylcarbamoyl) methyl]amine-1,4-naphthoquinone 17 was the best as inhibitor of beta-hematin formation with an Cl50 of 6.07 mM. These studies open up the novel possibility of development of 3-chloro-2Naminesubstituted- 1,4-naftoquinonas derivatives as potentials antimalarials that target beta-hematin formation and the inhibition of the development of cultured P. falciparum parasites, which should help delay the rapid onset of resistance to drugs acting at only a single site. These compounds represent a new family of promising antimalarials. |
| URI: | http://hdl.handle.net/10872/3868 |
| Appears in Collections: | Artículos Publicados |
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