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Inhibition of Helicobacter pylori aminoacyl-tRNA amidotransferase by chloramphenicol analogs.

Abstract：

:Genomic studies revealed the absence of glutaminyl-tRNA synthetase and/or asparaginyl-tRNA synthetase in many bacteria and all known archaea. In these microorganisms, glutaminyl-tRNA(Gln) (Gln-tRNA(Gln)) and/or asparaginyl-tRNA(Asn) (Asn-tRNA(Asn)) are synthesized via an indirect pathway involving side chain amidation of misacylated glutamyl-tRNA(Gln) (Glu-tRNA(Gln)) and/or aspartyl-tRNA(Asn) (Asp-tRNA(Asn)) by an amidotransferase. A series of chloramphenicol analogs have been synthesized and evaluated as inhibitors of Helicobacter pylori GatCAB amidotransferase. Compound 7a was identified as the most active competitive inhibitor of the transamidase activity with respect to Asp-tRNA(Asn) (K(m)=2μM), with a K(i) value of 27μM.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Balg C,De Mieri M,Huot JL,Blais SP,Lapointe J,Chênevert R

doi

10.1016/j.bmc.2010.09.045

subject

Has Abstract

pub_date

2010-11-15 00:00:00

pages

7868-72

issue

22

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(10)00882-5

journal_volume

18

pub_type

杂志文章

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