In vivo activity of an azole series of CCR2 antagonists

…, C Brooks, A Emmons, PJ Gough, C Mookherjee…

Index: Smethurst, Chris A.; Bevan, Nicola; Emmons, Amanda; Mookherjee, Claudette; Moores, Kitty; Peace, Simon; Piercy, Val; Watson, Steve P.; Zippoli, Mara; Brooks, Carl; Gough, Peter J.; Philp, Joanne Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7252 - 7255,4 Title/Abstract Full Text Show Details Smethurst, Chris A.; Bevan, Nicola; Brooks, Carl; Emmons, Amanda; Gough, Peter J.; Mookherjee, Claudette; Moores, Kitty; Peace, Simon; Philp, Joanne; Piercy, Val; Watson, Steve P.; Zippoli, Mara Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7252 - 7255

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Abstract

A number of patents and peer-reviewed publications have appeared that detail the development of small-molecule CCR2 antagonists 4 and representative series are displayed in Figure 1. A number of related series containing a basic centre have been reported, for example cyclohexylamines represented by 1 5 (Incyte), cyclopentylamines 2 6 and related structures 7 (Merck). Conversely, acidic CCR2 antagonists such as 3 have been described by researchers at ...