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Proteolytic stability assessed as alpha chymotrypsin (unknown origin)-mediated compound degradation after 24 hrs by RP-HPLC analysis

PubChem AID
1156577
Primary Citation
Antibacterial evaluation of structurally amphipathic, membrane active small cationic peptidomimetics: synthesized by incorporating 3-amino benzoic acid as peptidomimetic element [PMID: 24953028]
Source
External ID
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2015-04-04
  • Modify:
    2022-03-18
Description
This bioassay record (AID 1156577) reports results from the above primary citation. Additional data from the same publication are reported in a total of 31 BioAssay records in PubChem.

1 Description

Title: Antibacterial evaluation of structurally amphipathic, membrane active small cationic peptidomimetics: synthesized by incorporating 3-amino benzoic acid as peptidomimetic element.

Abstract: A new series of small cationic peptidomimetics were synthesized by incorporating 3-amino benzoic acid (3-ABA) in a small structural framework with the objective to mimic essential properties of natural antimicrobial peptides (AMPs). The new design approach resulted into improvement of activity and selectivity in comparison to linear peptides and allowed us to better understand the influence of structural amphipathicity on biological activity. Lead peptidomimetics displayed antibacterial activities against resistant pathogens (MRSA & MRSE). A calcein dye leakage experiment revealed a membranolytic effect of 4g and 4l which was further confirmed by fluorescence microscopy. In addition, proteolytic stability and no sign of resistance development against Staphylococcus aureus and MRSA demonstrate their potential for further development as novel antimicrobial therapeutics.

2 Comment

Journal: Eur J Med Chem

Year: 2014

Volume: 83

First Page: 102

Last Page: 115

DOI: 10.1016/j.ejmech.2014.06.023

3 Result Definitions

4 Data Table

6 Identity

6.1 BioAssay Name

Proteolytic stability assessed as alpha chymotrypsin (unknown origin)-mediated compound degradation after 24 hrs by RP-HPLC analysis

6.2 Source

6.3 External ID

6.4 Project Category

Literature, Extracted

6.5 Deposit Date

2015-04-04

6.6 Modify Date

Version 1.1
Version 2.1
Version 3.1
Version 4.1
2022-03-18 (currently shown)

6.7 Status

Live

7 Same-Publication BioAssays

8 BioAssay Annotations

Assay Type
ADME
Assay Organism

9 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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