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Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors.

Abstract：

:A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 = 0.2 microM) and activity against gram-positive organisms (MIC's = 0.015-0.06 microg/mL).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Tran TP,Ellsworth EL,Sanchez JP,Watson BM,Stier MA,Showalter HD,Domagala JM,Shapiro MA,Joannides ET,Gracheck SJ,Nguyen DQ,Bird P,Yip J,Sharadendu A,Ha C,Ramezani S,Wu X,Singh R

doi

10.1016/j.bmcl.2006.12.005

subject

Has Abstract

pub_date

2007-03-01 00:00:00

pages

1312-20

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)01399-0

journal_volume

17

pub_type

杂志文章

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