Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase

Elizabeth Fullam; Areej Abuhammad; David L Wilson; Matthew C Anderton; Steve G Davies; Angela J Russell; Edith Sim

doi:10.1016/j.bmcl.2010.12.099

Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase

Bioorg Med Chem Lett. 2011 Feb 15;21(4):1185-90. doi: 10.1016/j.bmcl.2010.12.099. Epub 2010 Dec 24.

Authors

Elizabeth Fullam¹, Areej Abuhammad, David L Wilson, Matthew C Anderton, Steve G Davies, Angela J Russell, Edith Sim

Affiliation

¹ Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK.

PMID: 21251821
DOI: 10.1016/j.bmcl.2010.12.099

Abstract

The synthesis and inhibitory potencies of a novel series of β-amino alcohols, based on the hit-compound 3-[3'-(4''-cyclopent-2'''-en-1'''-ylphenoxy)-2'-hydroxypropyl]-5,5 dimethylimidazolidine-2,4-dione as specific inhibitors of mycobacterial N-acetyltransferase (NAT) enzymes are reported. Effects of synthesised compounds on growth of Mycobacterium tuberculosis have been determined.

MeSH terms

Amino Alcohols / chemical synthesis
Amino Alcohols / chemistry*
Amino Alcohols / pharmacology
Antitubercular Agents / chemical synthesis
Antitubercular Agents / chemistry*
Antitubercular Agents / pharmacology
Arylamine N-Acetyltransferase / antagonists & inhibitors*
Arylamine N-Acetyltransferase / metabolism
Binding Sites
Catalytic Domain
Computer Simulation
Mycobacterium / drug effects
Mycobacterium / enzymology
Structure-Activity Relationship

Substances

Amino Alcohols
Antitubercular Agents
Arylamine N-Acetyltransferase