215311-41-4Relevant academic research and scientific papers
Multi-Institution Research and Education Collaboration Identifies New Antimicrobial Compounds
Fuller, Amelia A.,Dounay, Amy B.,Schirch, Douglas,Rivera, Daniel G.,Hansford, Karl A.,Elliott, Alysha G.,Zuegg, Johannes,Cooper, Matthew A,Blaskovich, Mark A. T.,Hitchens, Jacob R.,Burris-Hiday, Sarah,Tenorio, Kristiana,Mendez, Yanira,Samaritoni, J. Geno,O'Donnell, Martin J.,Scott, William L.
, p. 3187 - 3196 (2020)
New antibiotics are urgently needed to address increasing rates of multidrug resistant infections. Seventy-six diversely functionalized compounds, comprising five structural scaffolds, were synthesized and tested for their ability to inhibit microbial growth. Twenty-six compounds showed activity in the primary phenotypic screen at the Community for Open Antimicrobial Drug Discovery (CO-ADD). Follow-up testing of active molecules confirmed that two unnatural dipeptides inhibit the growth of Cryptococcus neoformans with a minimum inhibitory concentration (MIC) ≤ 8 μg/mL. Syntheses were carried out by undergraduate students at five schools implementing Distributed Drug Discovery (D3) programs. This report showcases that a collaborative research and educational process is a powerful approach to discover new molecules inhibiting microbial growth. Educational gains for students engaged in this project are highlighted in parallel to the research advances. Aspects of D3 that contribute to its success, including an emphasis on reproducibility of procedures, are discussed to underscore the power of this approach to solve important research problems and to inform other coupled chemical biology research and teaching endeavors.
Amino acid derivatives inhibiting extracellular matrix metalloproteinase and TNF alpha release
-
Page column 45, (2010/11/29)
The invention concerns compounds of general formula (X) in which Y represents in particular —CONHOH, R1represents in particular a C1-C5alkyl group, AA represents an amino acid, or an amino acid sequence, and R3represents in particular a group of formula —NH—(CH2)2—SCH3. The invention also concerns the pharmaceutical compositions containing them, and the methods for obtaining them.
