Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors

Bioorganic & Medicinal Chemistry
2009.0

Abstract

Herein we report a series of novel chloramphenicol amine derivatives as aminopeptidase N (APN)/CD13 inhibitors. All compounds were synthesized starting from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol. The preliminary biological screening showed that some compounds exhibited potent inhibitory activity against APN. It should be noted that one compound, 13b (IC(50)=7.1 microM), possess similar APN inhibitory activity compared with Bestatin (IC(50)=3.0 microM).

Knowledge Graph

Similar Paper

Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors
Bioorganic & Medicinal Chemistry 2009.0
Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine
Bioorganic & Medicinal Chemistry 2011.0
Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2011.0
Design, synthesis, and QSAR studies of novel lysine derives as amino-peptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2008.0
Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-l-aspartic acid as inhibitors of aminopeptidase N/CD13
Bioorganic & Medicinal Chemistry 2009.0
Design, synthesis and biological evaluation of novel amino acid ureido derivatives as aminopeptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2012.0
Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2009.0
Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors
Bioorganic & Medicinal Chemistry 2009.0
Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)
Bioorganic & Medicinal Chemistry 2008.0
Novel leucine ureido derivatives as aminopeptidase N inhibitors. Design, synthesis and activity evaluation
European Journal of Medicinal Chemistry 2016.0