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Photoactivated 2,3-distyrylindoles kill multi-drug resistant bacteria.

Abstract：

:Compounds based on the 2,3-distyrylindole scaffold were found to exhibit bactericidal properties upon irradiation with white light. At the concentration of 1 μM, the lead compound 1 completely (ca. 109 CFU/mL) eradicated such Gram-positive organisms as S. aureus (MRSA, MSSA), E. faecalis (VRE), S. pyogenes and S. mutans when irradiated with white light for 2 min. At the concentration of 5 μM and in the presence of polymyxin E at non-bactericidal 1.25 μg/mL concentration, 1 also showed a 7-log to 9-log reductions in bacterial counts of such Gram-negative organisms as multi-drug resistant (MDR) A. baumannii, MDR P. aeruginosa, E. coli and Klebsiella pneumoniae (CRE: KPC and NDM-1), also when irradiated with white light for 2 min. The structure-activity relationship studies revealed that unsubstituted at benzene rings 2,3-distyrylindole 2 was most potent and gave a 5-order of magnitude eradication of a MRSA strain at the concentration of 30 nM upon irradiation with white light. Initial mechanistic experiments revealed the disruption of bacterial cell membrane, but indicated that singlet oxygen production, which is commonly associated with photodynamic therapy, may not play a role in the bactericidal effects of the 2,3-distyrylindoles.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Edwards L,Turner D,Champion C,Khandelwal M,Zingler K,Stone C,Rajapaksha RD,Yang J,Ranasinghe MI,Kornienko A,Frolova LV,Rogelj S

doi

10.1016/j.bmcl.2018.04.001

subject

Has Abstract

pub_date

2018-06-01 00:00:00

pages

1879-1886

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30300-7

journal_volume

28

pub_type

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