TY - JOUR
T1 - Biphenyl-based analogues of thiolactomycin, active against Mycobacterium tuberculosis mtFabH fatty acid condensing enzyme
AU - Senior, Suzanne
AU - Illarionov, Petr
AU - Gurcha, Sudagar
AU - Campbell, IB
AU - Schaeffer, ML
AU - Minnikin, David
AU - Besra, Gurdyal
PY - 2003/11/3
Y1 - 2003/11/3
N2 - Analogues of the antibiotic thiolactomycin, with biphenyl-based 5-substituents, were found to have excellent in vitro inhibitory activity against the recombinant Mycobacterium tuberculosis beta-ketoacyl-ACP synthase mtFabH condensing enzyme. In particular, 5-(4'-benzyloxy-biphen-4-ylmethyl)-4-hydroxy-3,5-dimethyl-5H-thiophen-2- one exhibited approximately a 4-fold increased potency against this key condensing enzyme involved in M. tuberculosis mycolic acid biosynthesis, compared to thiolactomycin. (C) 2003 Elsevier Ltd. All rights reserved.
AB - Analogues of the antibiotic thiolactomycin, with biphenyl-based 5-substituents, were found to have excellent in vitro inhibitory activity against the recombinant Mycobacterium tuberculosis beta-ketoacyl-ACP synthase mtFabH condensing enzyme. In particular, 5-(4'-benzyloxy-biphen-4-ylmethyl)-4-hydroxy-3,5-dimethyl-5H-thiophen-2- one exhibited approximately a 4-fold increased potency against this key condensing enzyme involved in M. tuberculosis mycolic acid biosynthesis, compared to thiolactomycin. (C) 2003 Elsevier Ltd. All rights reserved.
UR - http://www.scopus.com/inward/record.url?scp=0141433395&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2003.08.015
DO - 10.1016/j.bmcl.2003.08.015
M3 - Article
C2 - 14552758
SN - 0960-894X
VL - 13
SP - 3685
EP - 3688
JO - Bioorganic & Medicinal Chemistry Letters
JF - Bioorganic & Medicinal Chemistry Letters
ER -
