1029520-96-4Relevant academic research and scientific papers
The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists
Porter, David W.,Bradley, Michelle,Brown, Zarin,Canova, Riccardo,Charlton, Steven,Cox, Brian,Hunt, Peter,Kolarik, David,Lewis, Sarah,O'Connor, Des,Reilly, John,Spanka, Carsten,Tedaldi, Lauren,Watson, Simon J.,Wermuth, Roland,Press, Neil J.
, p. 72 - 76 (2014/01/17)
A hit-to-lead optimisation programme was carried out on the Novartis archive screening hit, pyrazolopyrimidine 2-methyl-5-((phenylthio)methyl) pyrazolo[1,5-a]pyrimidin-7-ol 1, resulting in the discovery of CXCR2 receptor antagonist 2-benzyl-5-(((2,3-difluorophenyl)thio)methyl)-[1,2,4]triazolo[1,5-a] pyrimidin-7-ol 14. The SAR was investigated by systematic variation of the pendant thiol, alkyl and pyrimidinol groups. Replacement of the pyrazolopyrimidine core with a triazolo alternative led to a dual series of antagonists with favourable biological and pharmacokinetic properties.
5-SULFANYLMETHYL-[1,2,4] TRIAZOL[l,5-A] PYRIMIDIN-7-OL DERIVATIVES AS CXCR2 ANTAGONISTS
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Page/Page column 16; 17, (2008/12/05)
The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.
