Author/Authors :
Purakkattle Biju، نويسنده , , Arthur Taveras، نويسنده , , Younong Yu، نويسنده , , Junying Zheng، نويسنده , , Jianhua Chao، نويسنده , , Diane Rindgen، نويسنده , , James Jakway، نويسنده , , R. William Hipkin، نويسنده , , James Fossetta، نويسنده , , Xuedong Fan، نويسنده , , Jay Fine، نويسنده , , Hongchen Qiu، نويسنده , , J. Robert Merritt، نويسنده , , John J. Baldwin، نويسنده ,
Abstract :
A series of novel and potent 3,4-diamino-2,5-thiadiazole-1-oxides were prepared and found to show excellent binding affinities for CXCR2 and CXCR1 receptors and excellent inhibitory activity of Gro-α and IL-8 mediated in vitro hPMN MPO release of CXCR2 and CXCR1 expressing cell lines. On the other hand, a closely related 3,4-diamino-2,5-thiadiazole-dioxide did not show functional activity despite its excellent binding affinities for CXCR2 and CXCR1 in membrane binding assays. A detailed SAR has been discussed in these two closely related structures.
