AI Article Synopsis

  • AATSC is a compound with strong antimicrobial properties due to its unique chemical structure, which may resemble components of drug-like molecules.
  • AATSC acts as an uncompetitive inhibitor of the enzyme bovine liver dihydrofolate reductase, indicating its potential to block specific enzyme functions.
  • Additionally, AATSC improves the effectiveness of the cancer drug methotrexate, suggesting it could be beneficial in enhancing therapeutic treatments.

Article Abstract

N4-(2-Acetoxyethoxymethyl)-2-acetylpyridine thiosemicarbazone (AATSC) belongs to a series of molecules known to have broad antimicrobial inhibitory activity. These molecules contain the 2-acetoxyethoxy moiety which could conceivably take up a conformation analogous to that of the ribosyl group. Moreover, the thiosemicarbazone moiety, when in the presence of a suitable enzymatic site, could mimic the triazine group, which is found in a number of antifolate drugs. AATSC, which has both bacterial inhibitory activity and water solubility, was accordingly evaluated for its antifolate activity against the bovine liver dihydrofolate reductase. AATSC is shown to be a fully uncompetitive inhibitor of that enzyme. Furthermore, AATSC enhances the activity of methotrexate. Such a potentiation could be useful for therapeutic purposes.

Download full-text PDF

Source
http://dx.doi.org/10.1016/0304-4165(90)90156-qDOI Listing

Publication Analysis

Top Keywords

dihydrofolate reductase
8
n4-2-acetoxyethoxymethyl-2-acetylpyridine thiosemicarbazone
8
inhibitory activity
8
inhibition bovine
4
bovine dihydrofolate
4
reductase enhancement
4
enhancement methotrexate
4
methotrexate sensitivity
4
sensitivity n4-2-acetoxyethoxymethyl-2-acetylpyridine
4
thiosemicarbazone n4-2-acetoxyethoxymethyl-2-acetylpyridine
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!