Analysis of β-amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase.
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.
Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK.
Elizabeth
E
Fullam
Areej
A
Abuhammad
David L
DL
Wilson
Matthew C
MC
Anderton
Steve G
SG
Davies
Angela J
AJ
Russell
Edith
E
Sim
D000605:Amino Alcohols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001191:Arylamine N-Acetyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D001665:Binding Sites; D020134:Catalytic Domain; D003198:Computer Simulation; D009161:Mycobacterium / Q000187:drug effects / Q000201:enzymology; D013329:Structure-Activity Relationship
D000605:Amino Alcohols; D000995:Antitubercular Agents; D001191:Arylamine N-Acetyltransferase