3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists |
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Authors: | Biju Purakkattle Taveras Arthur Yu Younong Zheng Junying Chao Jianhua Rindgen Diane Jakway James Hipkin R William Fossetta James Fan Xuedong Fine Jay Qiu Hongchen Merritt J Robert Baldwin John J |
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Affiliation: | Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. purakkattle.biju@spcorp.com |
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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-alpha 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. |
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