Yancheva, Denista and Cherneva, Emiliya and Quick, Markus and Mikhova, Bozhanka and Shivachev, Boris and Nikolova, Rosisa and Djordjevic, Aleksandra and Untergehrer, Monika and Juergenliemk, Guido and Kraus, Birgit and Smecerovic, Andrija (2015) Synthesis, Crystal Structure and Biological Activity Screening of Novel N-(alpha-Bromoacyl)-alpha-amino Esters Containing Valyl Moiety. ACTA CHIMICA SLOVENICA, 62 (3). pp. 689-699. ISSN 1318-0207, 1580-3155
Full text not available from this repository. (Request a copy)Abstract
Three novel N-(alpha-bromoacy1)-alpha-amino esters: methyl 2-(2-bromo-3-methylbutanamido)pentanoate (1), methyl 2-(2bromo-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.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | DYNAMIC KINETIC RESOLUTION; CHIRAL 1,4-MORPHOLIN-2,5-DIONE DERIVATIVES; ALPHA-GLUCOSIDASE INHIBITORS; ANTIMICROBIAL ACTIVITY; ANTIVIRAL ACTIVITY; IN-VITRO; 2 6-(PROPAN-2-YL)-4-METHYL-MORPHOLINE-2,5-DIONES; DIPEPTIDE DERIVATIVES; ORAL BIOAVAILABILITY; OCULAR DISPOSITION; N-(alpha-bromoacyl)-alpha-amino esters; X-ray structure; cytotoxicity; anti-inflammatory activity; antibacterial activity |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical Biology (Prof. Heilmann) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 29 Jul 2019 08:28 |
| Last Modified: | 29 Jul 2019 08:28 |
| URI: | https://pred.uni-regensburg.de/id/eprint/6187 |
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