2. Academic Validation
  3. Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production

Oroxylin A analogs exhibited strong inhibitory activities against iNOS-mediated nitric oxide (NO) production

  • Bioorg Med Chem Lett. 2012 Apr 1;22(7):2534-5. doi: 10.1016/j.bmcl.2012.01.135.
Tuan-Ahn N Pham 1,  Haiyan Che,  Phuong-Thuy T Phan,  Jae-Won Lee,  Sung-Soo Kim,  Haeil Park
Affiliations

Affiliation

  • 1 College of Pharmacy, Kangwon National University, Chunchon 200-701, Republic of Korea.
PMID: 22366656 DOI: 10.1016/j.bmcl.2012.01.135
Abstract

A number of oroxylin A analogs were prepared and evaluated for their inhibitory activities against iNOS-mediated nitric oxide (NO) production from LPS-stimulated BV2 cells. The analogs were synthesized from purchased 2'-hydroxy-4,5,6-trimethoxyacetophenone and aldehydes in 3 steps. Among the tested compounds, several analogs (3b, 3c, 3d, 3f) exhibited strong inhibitory activities. Especially, the analog with 4-nitrophenyl group (3b) showed stronger inhibitory activity (IC(50)=4.73 μM) than that of wogonin (IC(50)=7.80 μM).

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