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Synthesis and anti-enterovirus activity of new analogues of MDL-860.
Dobrikov, Georgi M; Slavchev, Ivaylo; Nikolova, Ivanka; Stoyanova, Adelina; Nikolova, Nadya; Mukova, Lucia; Nikolova, Rosica; Shivachev, Boris; Galabov, Angel S.
Afiliación
  • Dobrikov GM; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, bl. 9, Acad. G. Bonchev str., Sofia 1113, Bulgaria. Electronic address: gmdob@orgchm.bas.bg.
  • Slavchev I; Institute of Organic Chemistry with Centre of Phytochemistry, Bulgarian Academy of Sciences, bl. 9, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Nikolova I; Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, bl. 26, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Stoyanova A; Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, bl. 26, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Nikolova N; Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, bl. 26, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Mukova L; Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, bl. 26, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Nikolova R; Institute of Mineralogy and Crystallography, Bulgarian Academy of Sciences, bl. 107, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Shivachev B; Institute of Mineralogy and Crystallography, Bulgarian Academy of Sciences, bl. 107, Acad. G. Bonchev str., Sofia 1113, Bulgaria.
  • Galabov AS; Stephan Angeloff Institute of Microbiology, Bulgarian Academy of Sciences, bl. 26, Acad. G. Bonchev str., Sofia 1113, Bulgaria. Electronic address: galabov@microbio.bas.bg.
Bioorg Med Chem Lett ; 27(19): 4540-4543, 2017 10 01.
Article en En | MEDLINE | ID: mdl-28870395
ABSTRACT
A series of twelve novel compounds, analogues of antiviral agent MDL-860 were synthesized and their antiviral activity was evaluated in vitro against enteroviruses poliovirus 1 (PV1), Coxsackieviruses B1 (CVB1) and Coxsackieviruses B3 (CVB3). Compounds 14, 24 and 25 manifested strong antiviral effects against CVB1 and PV1 (SI values of 405 and 118 for CVB1 and PV1 respectively). In contrast to the wide anti-enteroviral activity of MDL-860, these three compounds were inactive against CVB3. Compounds 14, 24 and 25 along with MDL-860 were tested in vivo in mice infected with CVB1. Marked protective effects of compounds 14 and 24 were established, PI values of 50% and 33.3%, respectively. In addition, almost all of the tested compounds manifested very low toxicity.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Enterovirus / Infecciones por Enterovirus / Nitrilos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Antivirales / Enterovirus / Infecciones por Enterovirus / Nitrilos Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article