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

Autor:	Anurag Sharadendu, Saeed Ramezani, Martin A. Shapiro, H. D. Hollis Showalter, E. Themis Joannides, Xiujuan Wu, Judy Yip, Bird Paul, John M. Domagala, Brian M. Watson, Stephen J. Gracheck, Tuan P. Tran, Chan Ha, Rajeshwar Singh, Edmund L. Ellsworth, Michael Stier, Joseph P. Sanchez, Dai Q. Nguyen
Rok vydání:	2007
Předmět:	medicine.drug_class Stereochemistry Clinical Biochemistry Pharmaceutical Science Gram-Positive Bacteria Biochemistry DNA gyrase Inhibitory Concentration 50 Structure-Activity Relationship Drug Discovery medicine Topoisomerase II Inhibitors Potency Amines Molecular Biology Quinazolinones Antibacterial agent chemistry.chemical_classification biology Chemistry Topoisomerase Organic Chemistry Anti-Bacterial Agents Enzyme DNA Gyrase Enzyme inhibitor biology.protein Molecular Medicine Antibacterial activity Topoisomerase inhibitor
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 17:1312-1320
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2006.12.005
Popis:	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 (IC 50 = 0.2 μM) and activity against Gram-positive organisms (MIC’s = 0.015–0.06 μ g/mL).
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d4af73f438dba10d7f564e0a34ff3416 https://doi.org/10.1016/j.bmcl.2006.12.005 Zobrazit plný text záznamu Full Text from ScienceDirect