Setembro 2013 vol. 1 num. 1 - Brazilian Meeting on Organic Synthesis 2011

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Synthesis of hybrids compounds by Click Chemistry and their bioactivities

Valdomir, Guillermo ; Padrón, Juan Ignacio ; Saldaña, Jenny ; Padrón, José Manuel ; Serra, Gloria ; Manta, Eduardo ; Martín, Victor S. ; Davyt, Danilo ;

Abstract:

In this work, a collection of hybrid compounds of type 1 (Scheme 1) were synthesized by a convergent route as potential anthelmintic drugs. One fragment of the hybrids is an oxazole or thiazole prepared from a serine dipeptide. The other domain, are a dihydropyran obtained by Prins’s cyclization, functionally with ethynyl moiety by Corey-Fusch reaction. Both heterocycles were coupled using the Huisgen´s reaction by a triazol. Cytotoxicity of hybrids were evaluated by seven cellular lines and anthelmintic activity by Nippostrongilus brasiliensis assay.

Abstract:

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Palavras-chave: Hybrids, Click Chemistry, Anthelmintics,

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DOI: 10.5151/chempro-14bmos-R0081-1

Referências bibliográficas
  • [1] 1 Phillips, A. J., Uto, Y., Wipf, P., Reno, M. J., Williams D. R.; Org. Lett. 2(8) (2000), 1165-1168.
  • [2] 2 León, L. G., Miranda, P. O., Martin, V. S., Padrón, J. I., Padrón, J. M.; Bioorg. And Med. Chem. Lett. 17 (2007) 3087–3090.
  • [3] 3 Rostovtsev, V.V., Green, L.G., Fokin, V.V., Sharpless, K.B.; Angew. Chem. Int. Ed. 41 (2002), 2596-2599.
Como citar:

Valdomir, Guillermo; Padrón, Juan Ignacio; Saldaña, Jenny; Padrón, José Manuel; Serra, Gloria; Manta, Eduardo; Martín, Victor S.; Davyt, Danilo; "Synthesis of hybrids compounds by Click Chemistry and their bioactivities", p. 81 . In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 2318-4043, DOI 10.5151/chempro-14bmos-R0081-1

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