Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.

Abstract:

:Tuberculosis (TB) continues to remain one of the most threatening diseases in the world. With the emergence of multi-drug resistant (MDR) and extensively drug resistant (XDR) strains, the need to develop new therapies is dire. The syntheses of a focused library of hydroxamates and hydroxamic acids is described, as well as anti-TB activity in the microplate alamar blue assay (MABA). A number of compounds exhibited good activity against Mtb, with notable compounds exhibiting MIC values in the range of 20-0.71 μM. This work suggests that both hydroxamates and their free acids may be incorporated into more complex scaffolds and serve as potential leads for the development of anti-TB agents.

journal_name

Bioorg Med Chem Lett

authors

Majewski MW,Cho S,Miller PA,Franzblau SG,Miller MJ

doi

10.1016/j.bmcl.2015.04.099

subject

Has Abstract

pub_date

2015-11-01 00:00:00

pages

4933-4936

issue

21

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00444-8

journal_volume

25

pub_type

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