Design and synthesis of 1H-pyrazolo[3,4-c]pyridine derivatives as a novel structural class of potent GPR119 agonists.

Abstract Design and synthesis of a novel class of 1 H -pyrazolo[3,4- c ]pyridine GPR119 receptor agonists are described. Lead compound 4 was identified through the ligand-based drug design approach. Modification of the left-hand aryl group (R 1 ) and right-hand piperidine N-capping group (R 2 ) led to the identification of compound 24 as a single-digit nanomolar GPR119 agonist.