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

Denista Yancheva, Emiliya Cherneva, Markus Quick, Bozhanka Mikhova, Boris Shivachev, Rosica Nikolova, Aleksandra Djordjevic, Monika Untergehrer, Guido Jürgenliemk, Birgit Kraus, Andrija Smelcerovic

Abstract


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.


Keywords


N-(α-bromoacyl)-α-amino esters; X-ray structure; cytotoxicity; anti-inflammatory activity; antibacterial activity

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DOI: http://dx.doi.org/10.17344/acsi.2015.1418

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Copyright (c) 2015 Denista Yancheva, Emiliya Cherneva, Markus Quick, Bozhanka Mikhova, Boris Shivachev, Rosica Nikolova, Aleksandra Djordjevic, Monika Untergehrer, Guido Jürgenliemk, Birgit Kraus, Andrija Smelcerovic

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