Fused-Ring Oxazolopyrrolopyridopyrimidine Systems with Gram-Negative Activity

Yiyuan Chen; Jonathan G Moloney; Kirsten E Christensen; Mark G Moloney

doi:10.3390/antibiotics6010002

Fused-Ring Oxazolopyrrolopyridopyrimidine Systems with Gram-Negative Activity

Antibiotics (Basel). 2017 Jan 13;6(1):2. doi: 10.3390/antibiotics6010002.

Authors

Yiyuan Chen¹, Jonathan G Moloney², Kirsten E Christensen³, Mark G Moloney⁴

Affiliations

¹ Chemistry Research Laboratory, Department of Chemistry, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK. cyy412@126.com.
² Chemistry Research Laboratory, Department of Chemistry, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK. jonathan.moloney@stcatz.ox.ac.uk.
³ Chemistry Research Laboratory, Department of Chemistry, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK. kirsten.christensen@chem.ox.ac.uk.
⁴ Chemistry Research Laboratory, Department of Chemistry, University of Oxford, 12 Mansfield Road, Oxford OX1 3TA, UK. mark.moloney@chem.ox.ac.uk.

Abstract

Fused polyheterocyclic derivatives are available by annulation of a tetramate scaffold, and been shown to have antibacterial activity against a Gram-negative, but not a Gram-positive, bacterial strain. While the activity is not potent, these systems are structurally novel showing, in particular, a high level of polarity, and offer potential for the optimization of antibacterial activity.

Keywords: annulation; antibacterial; heteroaromatic; polyheterocycle; tetramate.