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 Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Cai MG,Wu Y,Chang Jdoi
10.1016/j.bmcl.2016.03.089subject
Has Abstractpub_date
2016-05-15 00:00:00pages
2517-2520issue
10eissn
0960-894Xissn
1464-3405pii
S0960-894X(16)30321-3journal_volume
26pub_type
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