| Literature DB >> 17196390 |
Tuan P Tran1, Edmund L Ellsworth, Joseph P Sanchez, Brian M Watson, Michael A Stier, H D Hollis Showalter, John M Domagala, Martin A Shapiro, E Themis Joannides, Stephen J Gracheck, Dai Q Nguyen, Paul Bird, Judy Yip, Anurag Sharadendu, Chan Ha, Saeed Ramezani, Xiujuan Wu, Rajeshwar Singh.
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).Entities:
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Year: 2006 PMID： 17196390 DOI： 10.1016/j.bmcl.2006.12.005
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823