Tryptoline-based benzothiazoles re-sensitize MRSA to β-lactam antibiotics.

Tryptoline-based benzothiazoles re-sensitize MRSA to β-lactam antibiotics.
Bioorg Med Chem. 2019 Sep 09;:115095
Authors: Wang X, Chen J, Wang W, Jaunarajs A, Wang X
Abstract
Resistance-modifying agents (RMAs) offer a promising solution to combat bacterial antibiotic resistance. Here we report the discovery and structure-activity relationships of a new class of RMAs with a novel tryptoline-based benzothiazole scaffold. Our most potent compound in this series (4ad) re-sensitizes multiple MRSA strains to cephalosporins at low concentrations (2 μg/mL) and has low mammalian cytotoxicity with a half growth inhibitory concentration (GI50) > 100 μg/mL in human cervical carcinoma (HeLa) cells. In addition, the same core scaffold with different substitutions also gives good antibacterial activity against MRSA.
PMID: 31521461 [PubMed - as supplied by publisher]

Source: Bioorganic and Medicinal Chemistry - September 8, 2019 Category: Chemistry Authors: Wang X, Chen J, Wang W, Jaunarajs A, Wang X Tags: Bioorg Med Chem Source Type: research