Novel boronic acid derivatives of bis(indolyl) methane as anti-MRSA agents. Issue 10 (15th May 2017)

• Record Type: Journal Article
• Authors: Mandal, Santi M.; Pegu, Rupa; Porto, William F.; Franco, Octavio L.; Pratihar, Sanjay
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 10(2017)
• Page Start: 2135
• Page End: 2138
• Publication Date: 2017-05-15
• Subjects: Bis(indolyl) methane -- MRSA -- New generation antibiotics -- Bacterial cell wall -- Leucyl-tRNA synthetase; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.03.070
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Highlights: MRSA associated infection is major concern to public health and difficult to control. New molecules with selective, multi-target activity are desirable as pharmaceuticals. Nature and position of aryl and indole moieties in bis(indolyl) methane are vital for activity. The developed boronic acid derivatives have a dual target mechanism of inhibition of cell wall synthesis and tRNAsynthase. Abstract: Towards the search for a new generation of antibiotics to control methicillin-resistant Staphylococcus aureus (MRSA), the design and synthesis of various bis indolyl methane (BIM) derivatives based on their different electron donor and acceptor properties of the substituents have been made, in which boronic acid derivatives of BIM are found to be active against MRSA. The observed evidence with the lead compound reveals their strong anti-MRSA activity, which paves the way of design and further development of a new generation antibiotics.