European Journal of Medicinal Chemistry
| العنوان: | European Journal of Medicinal Chemistry |
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| المؤلفون: | Barbosa, Ticiano Pereira, Silva, Fábio P. L., Lopes, Horacimone Mendes, Batista, Guilherme N., Silva, Thiago G. da, Silva, Tânia Maria Sarmento da |
| المصدر: | Repositório Institucional da UFBA Universidade Federal da Bahia (UFBA) instacron:UFBA |
| سنة النشر: | 2009 |
| مصطلحات موضوعية: | Baylis–Hillman adducts, Green chemistry, Leishmania chagasi, Artemia salina Leach |
| الوصف: | Texto completo: acesso restrito. p. 1726-1730 Submitted by Suelen Reis (suziy.ellen@gmail.com) on 2013-10-15T15:20:21Z No. of bitstreams: 1 1-s2.0-S0223523408001347-main.pdf: 235749 bytes, checksum: 313f9ca590ed91e5d01b798cd3017a31 (MD5) Made available in DSpace on 2013-10-15T15:20:21Z (GMT). No. of bitstreams: 1 1-s2.0-S0223523408001347-main.pdf: 235749 bytes, checksum: 313f9ca590ed91e5d01b798cd3017a31 (MD5) Previous issue date: 2009 We described a very efficient procedure to prepare seven aromatic compounds (1–7), a new class of antileishmanial substances, through Baylis–Hillman reaction (BHR). With one, all the Baylis–Hillman adducts were prepared in quantitative yields by reaction of the corresponding aromatic aldehydes in acrylonitrile at 0 °C in only 10–40 min reaction time. We present our results about the toxicities of these compounds evaluated on the microcrustaceous Artemia salina Leach. and against promastigote Leishmania chagasi. All substances evaluated in this work have showed high bioactivity. The 3-hydroxy-2-methylene-3-(4-bromopheny)propanenitrile (4) (LC50 = 30.9 μg/mL on A. salina; IC50 = 25.2 μM on L. chagasi) was the most active compound evaluated on A. salina Leach. and on promastigote L. chagasi. The 2-[hydroxy(pyridin-4-yl)methyl]acrylonitrile (7) (LC50 = 30.9 μg/mL on A. salina Leach.; IC50 = 4.8 μg/mL on L. chagasi) was also a very active substance evaluated in this work on promastigote L. chagasi. |
| اللغة: | English |
| DOI: | 10.1016/j.ejmech.2008.03.016 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=od______3056::4044b037c7b5d9a96ce73def0e2f7274 http://www.repositorio.ufba.br/ri/handle/ri/13235 |
| Rights: | OPEN |
| رقم الانضمام: | edsair.od......3056..4044b037c7b5d9a96ce73def0e2f7274 |
| قاعدة البيانات: | OpenAIRE |
| DOI: | 10.1016/j.ejmech.2008.03.016 |
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