Srinakharinwirot University; Northeastern University; Northeastern University; Ramkhamhaeng University; National Science & Technology Development Agency - Thailand; National Center Genetic Engineering & Biotechnology (BIOTEC); University of Wollongong
Type
Article
Source Title
BIOORGANIC & MEDICINAL CHEMISTRY
Year
2009
Volume
17
Issue
11
Page
3866-3872
Open Access
Green Accepted
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI
10.1016/j.bmc.2009.04.028
Format
PDF
Abstract
Conjugation of the NorA substrate berberine and the NorA inhibitor 5-nitro-2-phenyl-1H-indole via a methylene ether linking group gave the 13-substituted berberine-NorA inhibitor hybrid, 3. A series of simpler arylmethyl ether hybrid structures were also synthesized. The hybrid 3 showed excellent antibacterial activity (MIC Staphylococcus aureus, 1.7 mu M), which was over 382-fold more active than the parent antibacterial berberine, against this bacterium. This compound was also shown to block the NorA efflux pump in S. aureus. (C) 2009 Elsevier Ltd. All rights reserved.
The Thailand Research Fund [MRG 4980158]; Commission on Higher Education, Srinakharinwirot University; Ramkhamhaeng University, Thailand; University of Wollongong, Australia; Northeastern University, USA; NIH [1R01AI076372-01A2]; NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [R01AI076372] Funding Source: NIH RePORTER
