A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase

X Y Yu; J M Hill; G Yu; Y Yang; A F Kluge; D Keith; J Finn; P Gallant; J Silverman; A Lim

doi:10.1016/s0960-894x(00)00697-1

A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase

Bioorg Med Chem Lett. 2001 Feb 26;11(4):541-4. doi: 10.1016/s0960-894x(00)00697-1.

Authors

X Y Yu¹, J M Hill, G Yu, Y Yang, A F Kluge, D Keith, J Finn, P Gallant, J Silverman, A Lim

Affiliation

¹ Department of Medicinal Chemistry, Cubist Pharmaceuticals, Inc., Cambridge, MA 02139, USA. [email protected]

PMID: 11229766
DOI: 10.1016/s0960-894x(00)00697-1

Abstract

A series of quinoline inhibitors of C. albicans prolyl tRNA synthetase was identified. The most potent analogue, 2-(4-bromo-phenyl)-6-chloro-8-methyl-4-quinolinecarboxylic acid, showed IC50 = 5 nM (Ca. ProRS) with high selectivity over the human enzyme.

MeSH terms

Amino Acyl-tRNA Synthetases / antagonists & inhibitors*
Candida albicans / drug effects*
Candida albicans / enzymology
Enzyme Inhibitors / pharmacology*
Quinolines / pharmacology*
RNA, Transfer, Pro / biosynthesis*
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Quinolines
RNA, Transfer, Pro
Amino Acyl-tRNA Synthetases