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Novel small molecule inhibitors of MDR Mycobacterium tuberculosis by NMR fragment screening of antigen 85C.

Abstract：

:Protein target-based discovery of novel antibiotics has been largely unsuccessful despite rich genome information. Particularly in need are new antibiotics for tuberculosis, which kills 1.6 million people annually and shows a rapid increase in multiple-drug-resistant cases. By combining fragment-based drug discovery with early whole cell antibacterial screening, we discovered novel ligand-efficient inhibitors of multiple-drug resistant Mycobacterium tuberculosis (Mtb), which bind to the substrate site of the Mtb protein antigen 85C, hitherto unused in Mtb chemotherapy.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Scheich C,Puetter V,Schade M

doi

10.1021/jm100993z

subject

Has Abstract

pub_date

2010-12-09 00:00:00

pages

8362-7

issue

23

eissn

0022-2623

issn

1520-4804

journal_volume

53

pub_type

杂志文章

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