Synthesis, crystal structure and biological activity screening of novel N-(α-bromoacyl)-α-amino esters containing valyl moiety

Autor: Denista Yancheva, Emiliya Cherneva, Markus Quick, Bozhanka Mikhova, Boris Shivachev, Rosica Nikolova, Aleksandra Djordjevic, Monika Untergehrer, Guido Jürgenliemk, Birgit Kraus, Andrija Smelcerovic
Jazyk: angličtina
Rok vydání: 2015
Předmět:
Zdroj: Acta Chimica Slovenica, Vol 62, Iss 3, Pp 689-699 (2015)
Druh dokumentu: article
ISSN: 1318-0207
1580-3155
DOI: 10.17344/acsi.2015.1418
Popis: Three novel N-(α-bromoacyl)-α-amino esters, methyl 2-(2-bromo-3-methylbutanamido)pentanoate (1), methyl 2-(2-bromo-3-methylbutanamido)-2-phenylacetate (2) and methyl 2-(2-bromo-3-methylbutanamido)-3-phenylpropanoate (3) were synthesized. Single crystal X-ray diffraction data are reported for compounds 1 and 2. The cytotoxicity, anti-inflammatory and antibacterial activity of compounds 1-3 were investigated. Additionally, the physico-chemical properties of studied compounds were calculated and an in silico toxicological study of compounds 1-3 was performed. The low level of cytotoxicity and absence of antibacterial and anti-inflammatory activity of 1-3 in tested concentrations might be a beneficial prerequisite for their incorporation in prodrugs.
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