Benzoic acid and pyridine derivatives as inhibitors of Trypanosoma cruzi trans-sialidase.
Benzoic acid and pyridine derivatives inhibit recombinant trans-sialidase from Trypanosoma cruzi with I50 values between 0.4 and 1mM. The best compounds, 4-acetylamino-3-hydroxymethylbenzoic acid and 5-acetylamino-6-aminopyridine-2-carboxylic acid, provide new leads to inhibitors not containing the synthetically complex sialic acid structure. The weak inhibition by such compounds contrasts with their much stronger inhibition of neuraminidase from Influenza virus.
Neres
João
J
School of Pharmacy and Pharmaceutical Sciences, University of Manchester, Manchester, M13 9PL, UK.
Bonnet
Pascal
P
Edwards
Philip N
PN
Kotian
Pravin L
PL
Buschiazzo
Alejandro
A
Alzari
Pedro M
PM
Bryce
Richard A
RA
Douglas
Kenneth T
KT
D000818:Animals; D019817:Benzoic Acid / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006023:Glycoproteins / Q000037:antagonists & inhibitors*; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D009439:Neuraminidase / Q000037:antagonists & inhibitors*; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D021241:Spectrometry, Mass, Electrospray Ionization; D014349:Trypanosoma cruzi / Q000201:enzymology*
D004791:Enzyme Inhibitors; D006023:Glycoproteins; D011725:Pyridines; D019817:Benzoic Acid; C069715:trans-sialidase; D009439:Neuraminidase