Amphiphilic derivatives of (3β,17β)-3-hydroxyandrost-5-ene-17-carboxylic acid
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články
PubMed
29100780
DOI
10.1016/j.steroids.2017.10.011
PII: S0039-128X(17)30191-5
Knihovny.cz E-zdroje
- Klíčová slova
- Amphiphile, Antimicrobial activity, Cytotoxicity, Diamine, Polyamine, Steroid,
- MeSH
- androsteny chemická syntéza chemie farmakologie MeSH
- antibakteriální látky chemická syntéza chemie farmakologie MeSH
- Escherichia coli účinky léků patogenita MeSH
- kyseliny karboxylové chemická syntéza chemie farmakologie MeSH
- mikrobiální testy citlivosti MeSH
- polyaminy chemická syntéza chemie farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- androsteny MeSH
- antibakteriální látky MeSH
- kyseliny karboxylové MeSH
- polyaminy MeSH
A series of amphiphilic derivatives of (3β,17β)-3-hydroxyandrost-5-ene-17-carboxylic acid (1) with the polyamine spermine and three other diamines, 1,2-diaminoethane, piperazine and cadaverine, were synthesized and their antimicrobial activity and cytotoxicity were investigated. Among the target compounds, several ones showed antimicrobial activity on Gram positive and Gram negative microorganisms. The most active compounds were 20 (Streptococcus mutans CCM 7409, 3.125 µM), 16 (Streptococcus mutans CCM 7409, 12.5 µM) and 10d (Escherichia coli CCM 3954, 12.5 µM). In addition, compounds 5d, 10d, 13 and 20 displayed cytotoxicity on CEM (12.1 ± 2.1 µM, 7.6 ± 1.0 µM, 19.0 ± 0.4 µM and 5.9 ± 0.7 µM, respectively). Two additional compounds displayed medium cytotoxicity on CEM, 5a (34.6 ± 5.2 µM) and 5c (37.7 ± 5.9 µM). The compound 13 and 20 displayed high toxicity also on normal fibroblasts.
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