Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells

Sun, J; Cao, N; Zhang, XM; Yang, YS; Zhang, YB; Wang, XM; Zhu, HL

HERO ID

3539130

Reference Type

Journal Article

Year

2011

Language

English

PMID

21782456

HERO ID 3539130
In Press No
Year 2011
Title Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells
Authors Sun, J; Cao, N; Zhang, XM; Yang, YS; Zhang, YB; Wang, XM; Zhu, HL
Journal Bioorganic & Medicinal Chemistry
Volume 19
Issue 16
Page Numbers 4895-4902
Abstract A series of oxadiazole derivatives containing 1,4-benzodioxan (4a-4s) have been first synthesized for their potential immunosuppressive activity. Among the compounds, compound 4i showed the most potent biological activity against RAW264.7 cells (inhibition=37.66±2.34% for NO overproduction and IC(50)=0.05μM for iNOS). Docking simulation was performed to position compound 4i into the iNOS structure active site to determine the probable binding model. RT-PCR experiment results demonstrated that some of these compounds possessed good immunosuppressive activity against iNOS, especially for compound 4i. Therefore, compound 4i with potent inhibitory activity may be a potential agent.
Doi 10.1016/j.bmc.2011.06.061
Pmid 21782456
Wosid WOS:000293503000022
Is Certified Translation No
Dupe Override No
Is Public Yes
Language Text English