During the course of our CCR2 research program we discovered a series of novel 3-amino-azetidinyl glycinamides with potent antagonist activity.  Replacement of the terminal benzoyl amide bond with a quinazoline led to a divergence in the SAR from the original series.  Not only were carbinol substituents on the cyclohexane ring equipotent with their des-oxy analogs but we also found that the (hetero)aryl substituents on that position were not necessary for potent antagonist activity.  This observation launched a comprehensive medicinal chemistry campaign encompassing both a range of heterocyclic quinazoline surrogates and investigation of non aromatic substituents on the distal region of the pharmacophore which will be detailed herein.

Discovery of novel monoaryl CCR2 antagonists

244th National Meeting (2012)

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