Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase

A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginel...

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Detalhes bibliográficos
Autor principal: Rao, V. Mallikarjuna (author)
Outros Autores: Kumar, P. Mahesh (author), Rambabu, D. (author), Kapavarapu, Ravikumar (author), Rani, S. Shobha (author), Misra, Parimal (author), Pal, Manojit (author)
Formato: article
Idioma:eng
Publicado em: 2013
Assuntos:
Pyrimidinone
Alkyne
Iodine
Palladium
Chorismate mutase
Texto completo:http://hdl.handle.net/10316/26909
País:Portugal
Oai:oai:estudogeral.sib.uc.pt:10316/26909
Descrição
Resumo:A series of novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one (DHPM) derivatives were designed, synthesized and evaluated in vitro as potential inhibitors of chorismate mutase (CM). All these compounds were prepared via a multi-component reaction (MCR) involving sequential I2-mediated Biginelli reaction followed by Cu-free Sonogashira coupling. Some of them showed promising inhibitory activities when tested at 30 μM. One compound showed dose dependent inhibition of CM with IC50 value of 14.76 ± 0.54 μM indicating o-alkynylphenyl substituted DHPM as a new scaffold for the discovery of promising inhibitors of CM.

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