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Synthesis of new 3-phenylquinazolin-4(3H)-one derivatives as potent antibacterial agents effective against methicillin- and vancomycin-resistant Staphylococcus aureus (MRSA and VRSA).

Abstract：

:Occurrence of infections due to the drug resistant Staphylococcus aureus is on rise necessitating the need for rapid development of new antibacterial agents. In our present work, a series of new 3-phenylquinazolin-4(3H)-one derivatives were designed, synthesized and evaluated for their antibacterial activity against ESKAP (E. coli, S. aureus, K. pneumoniae, A. baumannii, P. aeroginosa) pathogen panel and pathogenic mycobacterial strains. The study revealed that compounds 4a, 4c, 4e, 4f, 4g, 4i, 4o and 4p exhibited selective and potent inhibitory activity against Staphylococcus aureus with MIC values in the range of 0.125-8 µg/mL. Further, the compounds 4c, 4e and 4g were found to be non toxic to Vero cells (CC50 = >10->100 µg/mL) and exhibited favourable selectivity index (SI = 40->200). The compounds 4c, 4e and 4g also showed potent inhibitory activity against various MDR-S. aureus including VRSA. The promising results obtained indicated the potential use of the above series of compounds as promising antibacterial agents for the treatment of multidrug resistant Staphylococcus aureus infections.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Gatadi S,Gour J,Kaul G,Shukla M,Dasgupta A,Akunuri R,Tripathi R,Madhavi YV,Chopra S,Nanduri S

doi

10.1016/j.bioorg.2018.08.012

subject

Has Abstract

pub_date

2018-12-01 00:00:00

pages

175-183

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(18)30590-X

journal_volume

81

pub_type

杂志文章

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