Synthesis and biological evaluation of 2-arylimino-3-pyridin-thiazolineone derivatives as antibacterial agents.

Abstract:

:With an intention to find more potent antibacterial agents, four halogen disubstituted thiazolineone derivatives (2a-d), five halogen monosubstituted thiazolineone derivatives (2e-i), and eleven 2-arylimino-3-pyridin-thiazolineone derivatives (2j-t) were synthesized and screened for their antibacterial activity, bactericidal activity, cytotoxicity, and erythrocyte hemolysis. Most of the synthesized derivatives showed antibacterial activity in inhibiting the growth of S. epidermidis and MRSA, and exhibited safety in the cytotoxicity study on the Vero cells and hemolytic activities test on healthy human erythrocytes. 2-Arylimino-3-pyridin-thiazolineone derivatives not only improved the clog P, but also showed potent antibacterial activity in inhibiting the growth of S. epidermidis and MRSA. In particularly, several compounds (2f, 2i, 2r and 2t) showed bactericidal activity, in which compound 2r displayed the best inhibitory capacity among the synthesized compounds, and further druggability research is on going.

journal_name

Bioorg Med Chem Lett

authors

Cai MG,Wu Y,Chang J

doi

10.1016/j.bmcl.2016.03.089

subject

Has Abstract

pub_date

2016-05-15 00:00:00

pages

2517-2520

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30321-3

journal_volume

26

pub_type

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