|
|||||
|
|
Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors |
|
| Authors: | Tran Tuan P Ellsworth Edmund L Sanchez Joseph P Watson Brian M Stier Michael A Showalter H D Hollis Domagala John M Shapiro Martin A Joannides E Themis Gracheck Stephen J Nguyen Dai Q Bird Paul Yip Judy Sharadendu Anurag Ha Chan Ramezani Saeed Wu Xiujuan Singh Rajeshwar |
| Affiliation: | Department of Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. tuan.tran@pfizer.com |
| 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). |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |